In order to obtain the key intermediate of vandetanib,4-chloro-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline was synthesized from methyl 4-[1-(tert-butoxycarbonyl) piperidin-4-ylmethoxy]-3-methoxybenzoate by ...In order to obtain the key intermediate of vandetanib,4-chloro-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline was synthesized from methyl 4-[1-(tert-butoxycarbonyl) piperidin-4-ylmethoxy]-3-methoxybenzoate by deprotection,methylation,nitration,reduction,ring formation and substitution reaction in an overall yield of 58%.The structures of the compound and its intermediates were determined by 1H NMR and MS.展开更多
1文献来源Middleton G,Palmer DH,Greenhalf W,et al.Vandetanib plus Gemcitabine versus placebo plus Gemcitabine in locally advanced or metastatic pancreatic carcinoma(ViP):A prospective,randomised,double blind,multicentr...1文献来源Middleton G,Palmer DH,Greenhalf W,et al.Vandetanib plus Gemcitabine versus placebo plus Gemcitabine in locally advanced or metastatic pancreatic carcinoma(ViP):A prospective,randomised,double blind,multicentre phase 2 trial[J].Lancet Oncol,2017,18(4):486-499.2证据水平1a。3背景吉西他滨单药疗法仍然是转移性胰腺癌患者的标准治疗方案。厄洛替尼是一种EGFR酪氨酸激酶抑制剂,与吉西他滨联合治疗局部进展期和转移性胰腺癌,能略改善患者的中位生存期。展开更多
文摘In order to obtain the key intermediate of vandetanib,4-chloro-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline was synthesized from methyl 4-[1-(tert-butoxycarbonyl) piperidin-4-ylmethoxy]-3-methoxybenzoate by deprotection,methylation,nitration,reduction,ring formation and substitution reaction in an overall yield of 58%.The structures of the compound and its intermediates were determined by 1H NMR and MS.
文摘1文献来源Middleton G,Palmer DH,Greenhalf W,et al.Vandetanib plus Gemcitabine versus placebo plus Gemcitabine in locally advanced or metastatic pancreatic carcinoma(ViP):A prospective,randomised,double blind,multicentre phase 2 trial[J].Lancet Oncol,2017,18(4):486-499.2证据水平1a。3背景吉西他滨单药疗法仍然是转移性胰腺癌患者的标准治疗方案。厄洛替尼是一种EGFR酪氨酸激酶抑制剂,与吉西他滨联合治疗局部进展期和转移性胰腺癌,能略改善患者的中位生存期。