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Bioequivalence study of abacavir/lamivudine(600/300-mg) tablets in healthy Thai volunteers under fasting conditions
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作者 Ekawan Yoosakul Jaturavit Vattanarongkup +4 位作者 Chutima Manamuti Bancha Chuasuwan Isariya Techatanawat Busarat Karachot Porranee Puranajoti 《Asian Journal of Pharmaceutical Sciences》 SCIE CAS 2016年第1期233-234,共2页
Abacavir/lamivudine is a combination of two synthetic nucleoside analogues which is indicated in antiretroviral combination therapy for the treatment of human immunodeficiency virus(HIV)infection in adults and adolesc... Abacavir/lamivudine is a combination of two synthetic nucleoside analogues which is indicated in antiretroviral combination therapy for the treatment of human immunodeficiency virus(HIV)infection in adults and adolescents[1].A generic product of abacavir/lamivudine has been developed with lower price by the Government Pharmaceutical Organization(GPO)to be an alternative choice of related physicians and patients who will gain access to the lower price medicines at the same quality and safety as the reference product. 展开更多
关键词 abacavir LAMIVUDINE BIOEQUIVALENCE LC-MS/MS Pharmacokinetics
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Changes in Bone Mineral Density through 96 Weeks in Antiretroviral-Naïve HIV-1 Infected Patients Receiving Abacavir/Lamivudine and Raltegravir in the SHIELD Trial
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作者 Linda Battalora Amy Thomas +2 位作者 Brian Wine Belinda Ha Benjamin Young 《World Journal of AIDS》 2014年第1期38-44,共7页
Decreased bone mineral density (BMD) and osteoporotic fractures are areas of increasing concern among HIV-infected persons. Particular concern is the rapid decline in BMD after initiation of antiretroviral treatment (... Decreased bone mineral density (BMD) and osteoporotic fractures are areas of increasing concern among HIV-infected persons. Particular concern is the rapid decline in BMD after initiation of antiretroviral treatment (ART). This report describes DEXA-assessed changes in BMD and body fat in a study of fifteen antiretroviral-na?ve adults initiating abacavir/lamivudine and raltegravir for 96 weeks. Median percent changes from baseline at weeks 48 and 96 in BMD were 0.29% and -0.11% (spine);-1.25% and -1.75% (left hip). Median percent changes from baseline in fat from baseline were -0.82% and -3.04% (trunk);2.12% and 2.01% (limb). In this pilot study, ABC/3TC + RAL treatment had limited impact on BMD and body fat. 展开更多
关键词 Bonedensity abacavir HIV INTEGRASE LAMIVUDINE RALTEGRAVIR
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Trizivir (Abacavir/Lamivudine/Zidovudine) plus Lopinavir/Ritonavir Induction Therapy Followed by Trizivir-Alone Maintenance for HIV-1-Infected Patients: A 96-Week Pilot Treatment Simplification Study
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作者 Joseph C. Gathe Dean T. Martin +5 位作者 M. Keith Rawlings Benjamin Daquioag John E. Fuchs Vanessa C. Williams Katrina L. Oie Gary E. Pakes 《World Journal of AIDS》 2012年第3期245-251,共7页
Objective: The purpose of this study was to investigate whether switching HIV-infected patients stabilized on Trizivir (abacavir 300 mg/lamivudine 150 mg/zidovudine 300 mg) plus lopinavir/ritonavir 400 mg/100mg twice ... Objective: The purpose of this study was to investigate whether switching HIV-infected patients stabilized on Trizivir (abacavir 300 mg/lamivudine 150 mg/zidovudine 300 mg) plus lopinavir/ritonavir 400 mg/100mg twice daily to Trizivir alone affects clinical efficacy and tolerability. Methods: This phase 4, open-label, pilot study was conducted over 96 weeks in 23 antiretroviral-na?ve, HIV-infected patients. Initially, these patients received induction therapy with Trizivir plus lopinavir/ritonavir 400 mg/100mg twice daily. Patients who achieved a viral load 3. Nineteen patients completed induction;of the four who did not, three were lost to follow-up and one withdrew due to gastrointestinal adverse events. In 14 induction completers who had viral load measurements taken at week 48, intent-to-treat: observed analysis showed a week 48 viral load 3 higher than the baseline count. Twelve patients completed the subsequent 48-week Trizivir-alone maintenance phase, of whom 11 (92%) achieved viral loads of both 3 above baseline. Trizivir-only maintenance was associated with fewer adverse events than the Trizivir-lopinavir/ritonavir induction phase and with improvement in total cholesterol, LDL-cholesterol, and triglycerides. Conclusions: Trizivir-alone maintenance after Trizivir-lopinavir/ritonavir induction maintained virologic and CD4+ cell response, and was associated with an improved adverse event and lipid profile. 展开更多
关键词 abacavir/Lamivudine/Zidovudine HIV-1 Infection Induction-Maintenance Strategy KALETRA Lopinavir/Ritonavir Trizivir
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abacavir 关键词:强过敏反应
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作者 许关煜(编译) 栾雪梅(编译) 《中国处方药》 2008年第7期20-20,共1页
为避免出现危及生命的不良事件,美国FDA近日要求临床医师在使用一种名为abacavir的药物之前,要对患者进行基因筛查。
关键词 abacavir 过敏反应 关键词 美国FDA 不良事件 临床医师 基因筛查
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Abacavir方案可以有效地治疗HIV感染
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作者 孔朝霞 《中国性病艾滋病防治》 2002年第1期63-63,共1页
欧洲和加拿大学者最近通过研究证实,用核苷类逆转录酶抑制剂abacavir取代三联抗逆转录病毒治疗方案中的蛋白酶抑制剂,能够有效地治疗HIV感染,并具有良好的耐受性。由于并非所有的HIV感染者都能耐受长期的蛋白酶抑制剂治疗方案,研究人员... 欧洲和加拿大学者最近通过研究证实,用核苷类逆转录酶抑制剂abacavir取代三联抗逆转录病毒治疗方案中的蛋白酶抑制剂,能够有效地治疗HIV感染,并具有良好的耐受性。由于并非所有的HIV感染者都能耐受长期的蛋白酶抑制剂治疗方案,研究人员开始探索用abacavir取代蛋白酶抑制剂的效果。他们以211名至少接受过为期6个月的蛋白酶抑制剂方案治疗、血浆HIV-1RNA浓度在可探测水平以下的HIV感染者为研究对象,随机将其分为两组:一组继续接受该方案治疗(106人),另一组则用abacavir取代蛋白酶抑制剂(105人), 展开更多
关键词 艾滋病 HIV abacavir方案 治疗
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Whole blood platelet aggregometry in HIV-infected patients on treatment with abacavir
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作者 Rosario Palacios Munoz Jose A.González-Correa +4 位作者 Josefa Ruiz Enrique Nuno Manuel Márquez Jose P.de la Cruz Jesús Santos 《Open Journal of Internal Medicine》 2012年第2期62-66,共5页
Purpose: To assess platelet activity in HIV-patients with and without antiretroviral therapy (ART), analysing the influence of the presence or absence of ABC in the regimen. Methods: Observational, pilot study, includ... Purpose: To assess platelet activity in HIV-patients with and without antiretroviral therapy (ART), analysing the influence of the presence or absence of ABC in the regimen. Methods: Observational, pilot study, including 30 asymptomatic HIV-patients: 20 on ART for at least 24 weeks and with undetectable HIV viral load - 10 on ABC, 10 on tenofovir (TDF) - and 10 na?ve patients, and a control group of 10 HIV-negative subjects. No subject was receiving drugs with antiagregant activity. Platelet activity was assessed by measuring time-dependent platelet aggregometry (electrical impedance on fasting whole blood), induced by ADP (1.25, 2.5 μM), collagen (0.5, 1 μg/mL), arachidonic acid (100, 200 μM), and U46619 (receptor agonist of the tromboxano A2) (1.25, 2.5 μM). Statistic program: SPSS, 16.0. Results: Demographic, anthropometric data, and cardiovascular risk factors were similar in all groups, but older age and longer time of HIV infection in the ABC group (50.4 vs 36.1, 34.2 and 42.7 years, respectively;p < 0.05, and 140.3 vs 88.1 and 48.3 months in the two other groups of HIV patients;p < 0.05). Mean CD4 cells count was 564/mm3. Platelet aggregation with exposure to U46619 was higher in the ABC compared with the TDF group (11.1 vs 4.4%;p = 0.007), na?ve patients (11.1 vs 5.7%;p = 0.014), and the HIV-negative group (11.1 vs 6.5%;p = 0.04). These differences remained significant when controlled for age and time of HIV infection. Conclusions: ABC increases platelet aggregability possibly in relation with the receptor of tromboxano. Wider studies are needed to confirm this hypothesis. 展开更多
关键词 Antiretroviral Therapy abacavir Cardiovascular Risk Platelet Activity
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抗病毒药——Abacavir
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作者 关旭俊 《国外新药介绍》 1999年第3期12-16,共5页
关键词 抗病毒药 abacavir 药效学 耐药性
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Abacavir方案可有效地治疗HIV感染
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作者 孔朝霞 《国外医学情报》 2001年第12期37-37,共1页
欧洲和加拿大学者最近通过研究证实,用核苷类逆转录酶抑制剂abacavir取代三联抗逆转录病毒治疗方案中的蛋白酶抑制剂,能够有效的治疗HIV感染,并具有良好的耐受性。由于并非所有的HIV感染者都能耐受长期的蛋白酶抑制剂治疗方案。
关键词 HIV感染 abacavir方案 治疗 蛋白酶抑制剂
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遗传药理学指标预测Abacavir的过敏性
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作者 孔朝霞 《国外医学情报》 2002年第12期29-30,共2页
在第9届逆转录病毒和机会性感染年度会议上,为论证遗传药理学的最新研究进展在临床上的应用潜力,有两个研究小组各自独立报道了一种可以预测HIV感染者处于abacavir过敏高危状态的遗传药理学指标。
关键词 遗传药理学 核苷类逆转录酶抑制剂 abacavir 过敏性
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12063 每日一次的拉米夫定/abacavir可行
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作者 徐欣(摘) 《国外药讯》 2005年第12期23-24,共2页
一项为期48周的Ⅱ期研究结果显示,在对使用过抗逆转录病毒药治疗的HIV感染患者进行治疗时,使用每天一次固定剂量配方的核苷逆转录酶抑制剂(NRTI)abacavir(Ⅰ)加拉米夫定(1amivudine)(Ⅱ)的合剂效果并不低于每天两次的(Ⅰ)... 一项为期48周的Ⅱ期研究结果显示,在对使用过抗逆转录病毒药治疗的HIV感染患者进行治疗时,使用每天一次固定剂量配方的核苷逆转录酶抑制剂(NRTI)abacavir(Ⅰ)加拉米夫定(1amivudine)(Ⅱ)的合剂效果并不低于每天两次的(Ⅰ)加每天一次的(Ⅱ)。 展开更多
关键词 abacavir 拉米夫定 每日一次 核苷逆转录酶抑制剂 抗逆转录病毒 Ⅱ期研究 感染患者 固定剂量 药治疗 HIV
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Studies on abacavir-induced hypersensitivity reaction:a successful example of translation of pharmacogenetics to personalized medicine 被引量:3
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作者 GUO YongLi SHI LeMing +3 位作者 HONG HuiXiao SU ZhenQiang FUSCOE James NING BaiTang 《Science China(Life Sciences)》 SCIE CAS 2013年第2期119-124,共6页
Abacavir is an effective nucleoside analog reverse transcriptase inhibitor used to treat human immunodeficiency virus(HIV) infected patients.Its main side effect is hypersensitivity reaction(HSR).The incidence of the ... Abacavir is an effective nucleoside analog reverse transcriptase inhibitor used to treat human immunodeficiency virus(HIV) infected patients.Its main side effect is hypersensitivity reaction(HSR).The incidence of the HSR is associated with ethnicity among patients exposed to abacavir,and retrospective and prospective studies show a significantly increased risk of abacavir-induced HSR in human leukocyte antigen(HLA)-B*57:01-carrying patients.Immunological studies indicated that abacavir interacts specifically with HLA-B*57:01 and changed the binding specificity between the HLA molecule and the HLA-presented endogenous peptide repertoire,leading to a systemic autoimmune reaction.HLA-B*57:01 screening,combined with patch testing,had clinically predictive value and cost-effective impact in reducing the incidence of abacavir-induced HSR regardless of the HLA-B*57:01 prevalence in the population.Therefore,the US Food and Drug Administration(FDA) and international HIV treatment guidelines recommend a routine HLA-B*57:01 screening prior to abacavir treatment to decrease false positive diagnosis and prevent abacavir-induced HSR.The studies of abacavir-induced HSR and the implementation of the HLA-B*57:01 screening in the clinic represent a successful example of the use of pharmacogenetics for personalized diagnosis and therapy. 展开更多
关键词 personalized medicine PHARMACOGENETICS drug safety abacavir hypersensitivity reaction (HSR) HLA-B*57:01 HLA-B*57-01 screening
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人体生物等效性临床试验风险伦理评估要点初探 被引量:5
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作者 钱薇 郑林海 +2 位作者 杨迪 叶方琴 杨劲 《中国临床药理学与治疗学》 CAS CSCD 2017年第9期1077-1080,共4页
人体生物等效性试验是评价制剂质量的重要指标。由于已有大量药物有效性和安全性的数据积累,因而其伦理风险往往容易被申办方和伦理委员会所忽视。本文列出了几个具体案例,对人体生物等效性试验中伦理风险提出了几个评估要点,包括:药品... 人体生物等效性试验是评价制剂质量的重要指标。由于已有大量药物有效性和安全性的数据积累,因而其伦理风险往往容易被申办方和伦理委员会所忽视。本文列出了几个具体案例,对人体生物等效性试验中伦理风险提出了几个评估要点,包括:药品说明书中的不良反应;种族差异;健康志愿者和适应症患者不良反应差异等,以期为人体等效性试验的伦理风险控制提供有益的参考。 展开更多
关键词 伦理 人体生物等效性试验 阿巴卡韦 来那度胺 单硝酸异山梨酯 氯氮平 伊马替尼
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阿巴卡韦的合成 被引量:3
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作者 王峥 施振华 周伟澄 《中国医药工业杂志》 CAS CSCD 北大核心 2007年第1期1-4,共4页
环戊二烯和乙醛酸经Diels-Alder环合、丁酰化、酶水解得(1R,4S,5R)-(–)-4-endo-4-羟基-2-氧杂二环[3.3.0]辛-7-烯-3-酮,再经LiAlH4还原、NaIO4氧化、NaBH4还原、乙酰化得(1R,2R)-2-乙酰氧基环戊-3-烯-1-甲醇乙酸酯,再经与2-氨基-6-环... 环戊二烯和乙醛酸经Diels-Alder环合、丁酰化、酶水解得(1R,4S,5R)-(–)-4-endo-4-羟基-2-氧杂二环[3.3.0]辛-7-烯-3-酮,再经LiAlH4还原、NaIO4氧化、NaBH4还原、乙酰化得(1R,2R)-2-乙酰氧基环戊-3-烯-1-甲醇乙酸酯,再经与2-氨基-6-环丙胺基-9H-嘌呤缩合、NaOH水解后制得抗艾滋病药物阿巴卡韦,总收率约3%(以乙醛酸计)。 展开更多
关键词 阿巴卡韦 抗病毒药 艾滋病 合成
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2-氨基-6-环丙胺基-9H-嘌呤的合成 被引量:2
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作者 周惠良 胡奇林 +1 位作者 赵庆山 刘万毅 《中国医药工业杂志》 CAS CSCD 北大核心 2008年第11期811-813,共3页
氰乙酸乙酯经亚硝化、与盐酸胍在乙醇钠存在下缩合闭环、Pd/C催化还原得2,4,5-三氨基-6-羟基嘧啶,与甲酸环合得鸟嘌呤,再经乙酰化、氯化、与环丙胺缩合得到抗病毒药阿巴卡韦中间体2-氨基-6-环丙胺基-9H-嘌呤,总收率约39%。
关键词 2-氨基-6-环丙胺基-9H-嘌呤 阿巴卡韦 中间体 合成
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抗艾滋病药物阿巴卡韦的合成 被引量:1
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作者 姚永波 冯文华 +3 位作者 张越 范愉 邓愉凤 王铁松 《河北工业科技》 CAS 2006年第1期27-30,共4页
针对阿巴卡韦(abacavir)作为抗艾滋病新药效果明显、需求量大,在查阅大量国外文献的基础上,对abacavir的作用、合成路线、市场前景等作了综述,并对其关键碳环中间体的合成路线进行了归纳。
关键词 艾滋病 阿巴卡韦 药物合成 外消旋
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Prevalence of Human Leukocyte Antigen HLA-B*5701 in HIV-1 Infected Individuals in Brazil 被引量:1
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作者 Claudinéia de Araújo Cristina Valetta de Carvalho +6 位作者 Miriam Estela de Souza Freire Amanda Yamaguti Ivens Cuiabano Scaff Fernando José de Souza Flávia Galindo Silvestre Silva Ricardo Sobhie Diaz Ismael Dale Cotrim Guerreiro da Silva 《Open Journal of Genetics》 2014年第1期56-62,共7页
This study was designed to establish the prevalence of HLA-B*5701 at HIV-1 infected individuals in Brazil. A total of 517 consecutive individuals were followed in this study from February 2009 through July 2011. The p... This study was designed to establish the prevalence of HLA-B*5701 at HIV-1 infected individuals in Brazil. A total of 517 consecutive individuals were followed in this study from February 2009 through July 2011. The presence of HLA-B*5701 was determined by Nested-PCR with HLA-B*57 and HLA-B*5701 sequence-specific primers (PCR-SSP). The expression of HLA-B*57 was negative in the 385 (74.5%) and positive in the 103 (19.9%) of infected individuals. Among these, the expression of HLA-B5701 was positive in the 29 (5.6%) of individuals. No demographic or ethnic differences were found between HLA-B*57/HLA-B*5701 HIV-1 negative patients, with a prevalence of Caucasians (57.1%) individuals. During the period of study, 68 patients were submited to an abacavir contain- ing regimen. The HLA-B*5701 allele was observed in 7 (10.3%) patients, with a significant incidence of Hypersensitivity reactions at 4 of them (p < 0.001). Conclusions: Although Brazilian population consists of a mixture of individuals of Caucasian, African and Native American genetic background, prevalence of HLA-B*5701 in this population is similar to the one found in pure Caucasians. 展开更多
关键词 IMMUNOGENETICS HUMAN IMMUNODEFICIENCY Virus HLA-B*5701 ANTIGEN HUMAN abacavir
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取代非环核苷混膦酸酯类衍生物的合成及生物活性
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作者 欧瑜 傅晓钟 +3 位作者 查雨锋 张顺 苏航 董永喜 《中国药科大学学报》 CAS CSCD 北大核心 2014年第6期649-656,共8页
为寻找抗乙肝病毒(HBV)取代非环核苷混膦酸酯有效的结构优化策略。以阿德福韦单L-氨基酸酯和单非甾体药物羧酸酯为先导化合物,结合核苷类似物阿巴卡韦与阿拉莫韦的结构特征,采用亚结构拼合原理设计并合成了6-取代嘌呤非环核苷膦酸单L-... 为寻找抗乙肝病毒(HBV)取代非环核苷混膦酸酯有效的结构优化策略。以阿德福韦单L-氨基酸酯和单非甾体药物羧酸酯为先导化合物,结合核苷类似物阿巴卡韦与阿拉莫韦的结构特征,采用亚结构拼合原理设计并合成了6-取代嘌呤非环核苷膦酸单L-氨基酸酯、单非甾体药物羧酸酯前药(9a^9l),其结构经1H NMR,ESI-MS,ESI-HRMS确证。采用HepG2 2.2.15细胞株、HK-2细胞株进行了目标化合物抗HBV活性以及肾细胞毒性评价。结果表明,化合物9a具有较强的抗病毒活性与作用选择性(EC500.48μmol/L,SI 763.72),具有较低的肾细胞毒性以及较高的化学与酶学稳定性,值得进一步深入研究。 展开更多
关键词 非环核苷膦酸 阿巴卡韦 阿拉莫韦 非甾体抗炎药 合成 抗病毒活性
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N-(叔丁氧羰基)-2-氮杂双环[2.2.1]庚-5-烯-3-酮的手性拆分
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作者 李普瑞 胡建建 +2 位作者 王晓川 张玲玲 王晓钟 《高校化学工程学报》 EI CAS CSCD 北大核心 2015年第5期1167-1170,共4页
(-)-(1R,4S)-N-(叔丁氧羰基)-2-氮杂双环[2.2.1]庚-5-烯-3-酮是抗艾滋病药物阿巴卡韦的重要中间体。今以2-氮杂双环[2.2.1]庚-5-烯-3-酮为原料,先与(Boc)2O反应生成外消旋体(±)-N-(叔丁氧羰基)-2-氮杂双环[2.2.1]庚-5-烯-3-酮,再... (-)-(1R,4S)-N-(叔丁氧羰基)-2-氮杂双环[2.2.1]庚-5-烯-3-酮是抗艾滋病药物阿巴卡韦的重要中间体。今以2-氮杂双环[2.2.1]庚-5-烯-3-酮为原料,先与(Boc)2O反应生成外消旋体(±)-N-(叔丁氧羰基)-2-氮杂双环[2.2.1]庚-5-烯-3-酮,再以固定化脂肪酶作为拆分试剂选择性拆分制得。试验中分别使用了三种酶,三种酶均表现出较好的反应活性和较高的反应收率,其中固定化酶Lipozyme RM IM的反应活性最高,对其催化的酶促反应进行了优化,得到最佳的反应条件:以异丙醚为反应溶剂,酶与底物质量投料比为1.5/2.0,反应温度为30℃,收率46.5%,对映体过量大于99%。结构经1H-NMR确证。该方法成本低,酶的选择性、催化活性和反应收率高。 展开更多
关键词 阿巴卡韦 N-(叔丁氧羰基)-2-氮杂双环[2.2.1]庚-5-烯-3-酮 固定化脂肪酶 手性拆分
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