有机化学人才网 | 最新人才 | 最新职位 | 技术交易 | 药物合成 |
   
全站搜索: |
  您当前位置:网站首页 >> 药物合成路线图解
 

药物详细合成路线

Name Moclobemide;Ro-11-1163;Moclamine;Manerix;Aurorix
Chemical Name 4-Chloro-N-[2-(4-morpholinyl)ethyl]benzamide
CAS 71320-77-9
Related CAS
Formula C13H17ClN2O2
Structure
Formula Weight 268.74564
Stage 上市-1990
Company Roche (Originator), Dainippon Pharmaceutical (Licensee)
Activity/Mechanism Antidepressants, Anxiolytics, Mood Disorders, Treatment of, PSYCHOPHARMACOLOGIC DRUGS, Social Phobia, Treatment for, MAO-A Inhibitors
Syn. Route 1
Route 1
this compound can be prepared in several different ways:1) by reaction of p-chlorobenzoyl chloride (i) with n-(2-aminoethyl)morpholine (ii) in pyridine.2) by reaction of p-chlorobenzoyl anhydride (iii) with n-(2-aminoethyl)morpholine (ii) in pyridine.3) by reaction of methyl p-chlorobenzoate (iv) with n-(2-aminoethyl)morpholine (ii) at 120 c.4) by reaction of n-(p-chlorobenzoyl)succinimide (v) with n-(2-aminoethyl)morpholine (ii) in dioxane.5) by reaction of p-nitrophenyl p-chlorobenzoate (vi) with n-(2-aminoethyl)morpholine (ii) in thf.6) by reaction of p-chloro-n-(2-chloroethyl)benzamide (vii) with morpholine (viii) at 100 c.7) by reaction of p-chlorobenzoylaziridine (ix) with morpholine (viii) in refluxing toluene.8) by reaction of p-chlorobenzaldehyde (x) with n-(2-aminoethyl)morpholine (ii) in refluxing benzene to give 4-[2-[(p-chlorobenzylidene)amino]ethyl]morpholine (xi), followed by an oxidation with h2o2 in methanol.9) by reaction of p-chloro-n-(2-morpholinoethyl)thiobenzamide (xii) with lead tetraacetate in refluxing water.11) by reaction of p-chlorobenzoic acid (xiv) with n-(2-aminoethyl)morpholine (ii) by means of dicyclohexylcarbodiimide in pyridine, or by means of chloroformic acid ethyl ester and triethylamine in acetone.10) by isomerization of (alpha-(p-chlorophenyl)-n-(2-morpholinoethyl)nitrone (xiii) in hot acetic acid - acetic anhydride, followed by a treatment with naoh.
List of intermediates No.
[(1s)-2-bromo-2-(bromomethyl)cyclopropyl]methyl acetate (i)
2-(4-benzhydryl-1-piperazinyl)ethyl (z)-2-acetyl-3-(3-nitrophenyl)-2-propenoate (viii)
4-amino-5-ethyl-4h-1,2,4-triazol-3-ylhydrosulfide; 4-amino-5-ethyl-4h-1,2,4-triazole-3-thiol (ii)
methyl 5-acetyl-2-[(2-oxotetrahydro-3-furanyl)oxy]benzoate (xiv)
n-(2-ethoxybenzyl)[3-(4-methylphenoxy)phenyl]methanamine; n-(2-ethoxybenzyl)-n-[3-(4-methylphenoxy)benzyl]amine (x)
(3s,6r,7r,8s,12z)-3-[[tert-butyl(dimethyl)silyl]oxy]-7-hydroxy-16-methoxy-4,4,6,8-tetramethyl-5-oxo-12-hexadecenoic acid (iii)
(3s,6s,7r,8s,12z)-3-[[tert-butyl(dimethyl)silyl]oxy]-7-hydroxy-16-methoxy-4,4,6,8-tetramethyl-5-oxo-12-hexadecenoic acid (iv)
(1e,3s)-2-methyl-1-(2-methyl-1,3-thiazol-4-yl)-1,5-hexadien-3-ol (v)
(1s)-1-[(e)-1-methyl-2-(2-methyl-1,3-thiazol-4-yl)ethenyl]-3-butenyl (3s,6s,7s,8s,12z)-3-[[tert-butyl(dimethyl)silyl]oxy]-7-hydroxy-16-methoxy-4,4,6,8-tetramethyl-5-oxo-12-hexadecenoate (vi)
(1s)-1-[(e)-1-methyl-2-(2-methyl-1,3-thiazol-4-yl)ethenyl]-3-butenyl (3s,6s,7r,8s,12z)-3-[[tert-butyl(dimethyl)silyl]oxy]-7-hydroxy-16-methoxy-4,4,6,8-tetramethyl-5-oxo-12-hexadecenoate (vii)
(1s)-1-[(e)-1-methyl-2-(2-methyl-1,3-thiazol-4-yl)ethenyl]-3-butenyl (3s,6r,7r,8s,12z)-3-[[tert-butyl(dimethyl)silyl]oxy]-7-hydroxy-16-methoxy-4,4,6,8-tetramethyl-5-oxo-12-hexadecenoate (ix)
(1s)-1-[(e)-1-methyl-2-(2-methyl-1,3-thiazol-4-yl)ethenyl]-3-butenyl (3s,6r,7s,8s,12z)-3-[[tert-butyl(dimethyl)silyl]oxy]-7-hydroxy-16-methoxy-4,4,6,8-tetramethyl-5-oxo-12-hexadecenoate (xi)
(4s,7r,8s,9s,16s)-4-[[tert-butyl(dimethyl)silyl]oxy]-8-hydroxy-5,5,7,9-tetramethyl-16-[(e)-1-methyl-2-(2-methyl-1,3-thiazol-4-yl)ethenyl]oxa-13-cyclohexadecene-2,6-dione (xii)
3-methyl-3-(trifluoromethyl)-1,2-dioxirane (xiii)
Reference 1:
    bukard, w.; wyss, p.c. (f. hoffmann-la roche ag); benzamides. be 0851422; ca 1076112; de 2706179; fr 2340940; gb 1512194; jp 52100476; nl 7701144; us 4210754; za 7700488 .
Reference 2:
    blancafort, p.; serradell, m.n.; castaner, j.; grau, m.; moclobemide. drugs fut 1983, 8, 2, 124.

来源:药化网

作者:药化小编

摘要:本文合成路线介绍的是药物中文名吗氯贝胺;英文名Moclobemide;Ro-11-1163;Moclamine;Manerix;Aurorix;CAS[71320-77-9]

 
推荐VIP企业
无锡景耀生物科技有限公司
杭州卢普生物科技有限公司
宁波赛伦化工有限公司
苏州昊赛生物科技有限公司
北京嘉盛扬医药科技有限公司
上海泽涵生物医药科技有限公司
河北固安三利化工公司
郑州凯普瑞生物技术有限公司
上海药谷药业有限公司
兰州康寓信生物科技有限公司
湖北朗昕生化药业有限公司
武汉福鑫化工有限公司
嘉兴市英南化工有限公司
苏州迪飞医药科技有限公司
北京富安凯科技有限公司
上海盛中医药化工有限公司
连云港天和化学有限公司
南京晨瑞医药科技有限公司
南京苏如化工有限公司
常州瑞盛化工有限公司
热门文章
丁酮市场高位僵持
山东地区辛醇市场走势整理
浙江地区醋酸价格
广东地区DMF市场动态
安徽地区甲醇市场盘整
山东地区顺酐市场行情整理
华南地区顺酐市场行情整理
华东苯酐市场价格平稳
华北地区BDO市场偏弱整理
华南地区顺酐市场行情整理
拜耳氟吡呋喃酮或将在我国首获正
山东地区辛醇市场保持稳定
华北地区邻苯市场行情暂稳
华南地区顺酐市场行情整理
华东苯酐市场价格平稳
山东地区辛醇市场保持稳定
黄山地区环氧氯丙烷动态
江西地区二氯甲烷价格暂稳
浙江地区二氯甲烷价格上调
山东地区辛醇市场行情
 友情链接
有机化学人才网  
首页 | 广告服务 | 建站服务 | 关于我们 | 联系我们 | 版权声明