A new method for the synthesis of ramosetron hydrochloride, the most wildly used 5-HT3 receptor antagonist, was reported. The intermediate 8 was obtained in a high e.e. value via lipase catalyzed hydrolytic kinetic re...A new method for the synthesis of ramosetron hydrochloride, the most wildly used 5-HT3 receptor antagonist, was reported. The intermediate 8 was obtained in a high e.e. value via lipase catalyzed hydrolytic kinetic resolution. Then enantiomerically pure ramosetron hydrochloride was synthesized in two steps with excellent yield （the total yield is 24.6%）. The method provides a new environment friendly and atom economy way to synthesize enantiomerically pure ramosetron.展开更多
Difloxacin hydrochloride, one of aryl-fluoro quinolone antibiotic, has been synthesized in seven steps from 2, 4-dichloro-5-fluoroacetophenone via oxalylation, ethoxymethylenation, amination, cyclization, hydrolysis, ...Difloxacin hydrochloride, one of aryl-fluoro quinolone antibiotic, has been synthesized in seven steps from 2, 4-dichloro-5-fluoroacetophenone via oxalylation, ethoxymethylenation, amination, cyclization, hydrolysis, decarbonylation and N-methylpiperazination. Additional four new intermediates are produced.展开更多
A convenient approach for the preparation of sarpogrelate hydrochloride was developed.Two series of sarpogrelate hydrochloride analogues were designed and synthesized in order to improve their platelet aggregation inh...A convenient approach for the preparation of sarpogrelate hydrochloride was developed.Two series of sarpogrelate hydrochloride analogues were designed and synthesized in order to improve their platelet aggregation inhibitory activities, biological tests suggested that these compounds have platelet aggregation inhibitory activities to some extent.展开更多
An efficient synthesis of novelα-aminophosphonates by the reaction of aldehydes and amines with triethyl phosphite in the presence of the easily available,inexpensive,and nontoxic catalyst thiamine hydrochloride（VB1...An efficient synthesis of novelα-aminophosphonates by the reaction of aldehydes and amines with triethyl phosphite in the presence of the easily available,inexpensive,and nontoxic catalyst thiamine hydrochloride（VB1）.This method affords theα-aminopho-sphonates under the influence of ultrasound irradiation in aqueous medium,in short reaction times（4-6 min）,high yields（85-95%）, with improved purity.The process is green,mild,inexpensive and excellent yields are the main compensation of this procedure.展开更多
A novel and simple procedure for the enantiospecific synthesis of penehyclidine hydrochloride （8018） isomers and the R configuration derivatives was described. The intramolecular asymmetric cyclization of the monosu...A novel and simple procedure for the enantiospecific synthesis of penehyclidine hydrochloride （8018） isomers and the R configuration derivatives was described. The intramolecular asymmetric cyclization of the monosulfonate of compound 1,2-diol was applied to the execution of the synthesis of the key chiral building block for the first time. The aimed products were obtained with moderate yield in〉99% ee.展开更多
Tilisolol hydrochloride 1, a non-selective β-adrenoceptor blocker, was developed as a drug for the treatment of hypertension and angina pectoris. The optical active forms of 1, la and lb were synthesized from inexpen...Tilisolol hydrochloride 1, a non-selective β-adrenoceptor blocker, was developed as a drug for the treatment of hypertension and angina pectoris. The optical active forms of 1, la and lb were synthesized from inexpensive phthalic anhydride 2 in eight steps with 13% （S） and 15% （R） overall yield.展开更多
A green and efficient synthesis of 3-pyrazolyl indoles was developed by the eye 1 ocondensation reactionof β-ethylthio-β-indolyl-α,β-unsaturated ketones with semi carbazide hydrochloride as hydrazine equivalent in...A green and efficient synthesis of 3-pyrazolyl indoles was developed by the eye 1 ocondensation reactionof β-ethylthio-β-indolyl-α,β-unsaturated ketones with semi carbazide hydrochloride as hydrazine equivalent in thepresence of 3 equiv. of PEG400(la/PEG mole ratio of 1:3) in reflux water. This procedure did not require toxichydrazine and product purification, eliminating the use of toxic liquid chemicals.展开更多
基金Supported by the National Natural Science Foundation of China(No.20802025)the Jilin Provincial Science & Technol-ogy Sustentation Program, China(Nos.20090585, 20100538)
文摘A new method for the synthesis of ramosetron hydrochloride, the most wildly used 5-HT3 receptor antagonist, was reported. The intermediate 8 was obtained in a high e.e. value via lipase catalyzed hydrolytic kinetic resolution. Then enantiomerically pure ramosetron hydrochloride was synthesized in two steps with excellent yield （the total yield is 24.6%）. The method provides a new environment friendly and atom economy way to synthesize enantiomerically pure ramosetron.
文摘Difloxacin hydrochloride, one of aryl-fluoro quinolone antibiotic, has been synthesized in seven steps from 2, 4-dichloro-5-fluoroacetophenone via oxalylation, ethoxymethylenation, amination, cyclization, hydrolysis, decarbonylation and N-methylpiperazination. Additional four new intermediates are produced.
文摘A convenient approach for the preparation of sarpogrelate hydrochloride was developed.Two series of sarpogrelate hydrochloride analogues were designed and synthesized in order to improve their platelet aggregation inhibitory activities, biological tests suggested that these compounds have platelet aggregation inhibitory activities to some extent.
文摘An efficient synthesis of novelα-aminophosphonates by the reaction of aldehydes and amines with triethyl phosphite in the presence of the easily available,inexpensive,and nontoxic catalyst thiamine hydrochloride（VB1）.This method affords theα-aminopho-sphonates under the influence of ultrasound irradiation in aqueous medium,in short reaction times（4-6 min）,high yields（85-95%）, with improved purity.The process is green,mild,inexpensive and excellent yields are the main compensation of this procedure.
基金Project supported by the National Natural Science Foundation of China （No. 203900508）.
文摘A novel and simple procedure for the enantiospecific synthesis of penehyclidine hydrochloride （8018） isomers and the R configuration derivatives was described. The intramolecular asymmetric cyclization of the monosulfonate of compound 1,2-diol was applied to the execution of the synthesis of the key chiral building block for the first time. The aimed products were obtained with moderate yield in〉99% ee.
基金supported by the National Natural Science Foundation of China(No.30672537)
文摘Tilisolol hydrochloride 1, a non-selective β-adrenoceptor blocker, was developed as a drug for the treatment of hypertension and angina pectoris. The optical active forms of 1, la and lb were synthesized from inexpensive phthalic anhydride 2 in eight steps with 13% （S） and 15% （R） overall yield.
基金Supported by the National Natural Science Foundation of China(No.20902010)the Foundation of Science and Technology Research Projects of the 13th Five-year Plan of Jilin Provincial Department of Education,China(No,2016037).
文摘A green and efficient synthesis of 3-pyrazolyl indoles was developed by the eye 1 ocondensation reactionof β-ethylthio-β-indolyl-α,β-unsaturated ketones with semi carbazide hydrochloride as hydrazine equivalent in thepresence of 3 equiv. of PEG400(la/PEG mole ratio of 1:3) in reflux water. This procedure did not require toxichydrazine and product purification, eliminating the use of toxic liquid chemicals.
