发明名称 MANUFACTURE OF N-ALKYLATED AMINO ACID AND ESTER OF SAME
摘要 For the Contracting states : BE, CH, DE, FR, GB, IT, LU, NL, SE 1. A process for preparing compounds of the formula I see diagramm : EP0117448,P21,F1 in which n = 1 or 2, R denotes, hydrogen, carboxy, carbamoyl, an optionally substituted aliphatic radical having 2-8 carbon atoms, an optionally substituted cycloaliphatic radical having 3-9 carbon atoms, an optionally substituted aromatic radical having 6-12 carbon atoms, an OR**4 or SR**4 radical in which R**4 represents an optionally substituted aliphatic radical having 1-4 carbon atoms, an optionally substituted aromatic radical having 6-12 carbon atoms or an optionally substituted heteroaromatic radical having 5-10 ring atoms, or an optionally substituted heteroaromatic radical having 5-10 ring atoms, R**1 denotes hydrogen, an optionally substituted aliphatic radical having 1-6 carbon atoms, an optionally substituted cycloaliphatic radical having 3-9 carbon atoms, an optionally substituted cycloaliphatic-aliphatic radical having 4-13 carbon atoms, an optionally substituted aromatic radical having 6-12 carbon atoms, an optionally substituted araliphatic radical having 7-16 carbon atoms, an optionally substituted heteroaromatic radical having 5-10 ring atoms or the side chain of an optionally protected naturally occuring alpha-amino acid, R**2 and R**3 are identical or different and denote hydrogen, an optionally substituted aliphatic radical having 1-6 carbon atoms, an optionally substituted cycloaliphatic radical having 3-9 carbon atoms, an optionally substituted cycloaliphatic-aliphatic radical having 4-12 carbon atoms, an optionally substituted aromatic radical having 6-12 carbon atoms or an optionally substituted araliphatic radical having 7-16 carbon atoms, which comprises reacting compounds of the formulae II ou III see diagramm : EP0117448,P22,F2 in which n, R, R**1, R**2 and R**3 have the abovementioned meanings, with compounds of the formulae IV or V see diagramm : EP0117448,P22,F3 in which R, R**1, R**2, R**3 and n have the abovementioned meanings, if desired eliminating ester groups by hydrolysis or if desired esterifying free carboxyl groups in a manner known per se. For the Contracting state : Austria 1. A process for preparing compounds of the formula see diagramm : EP0117448,P25,F1 in which n = 1 or 2, R denotes, carbamoyl, hydrogen, carboxy an optionally substituted aliphatic radical having 2-8 carbon atoms, an optionally substituted cycloaliphatic radical having 3-9 carbon atoms, an optionally substituted aromatic radical having 6-12 carbon atoms, an OR**4 or SR**4 radical in which R**4 represents an optionally substituted aliphatic radical having 1-4 carbon atoms, an optionally substituted aromatic radical having 6-12 carbon atoms or an optionally substituted heteroaromatic radical having 5-10 ring atoms, or an optionally substituted heteroaromatic radical having 5-10 ring atoms, R**1 denotes hydrogen, an optionally substituted aliphatic radical having 1-6 carbon atoms, an optionally substituted cycloaliphatic radical having 3-9 carbon atoms, an optionally substituted cycloaliphatic-aliphatic radical having 4-13 carbon atoms, an optionally substituted aromatic radical having 6-12 carbon atoms, an optionally substituted araliphatic radical having 7-16 carbon atoms, an optionally substituted heteroaromatic radical having 5-10 ring atoms or the side chain of an optionally protected naturally accuring alpha-amino acid, R**2 and R**3 are identical or different and denote hydrogen, an optionally substituted aliphatic radical having 1-6 carbon atoms, an optionally substituted cycloaliphatic radical having 3-9 carbon atoms, an optionally substituted cycloaliphatic-aliphatic radical having 4-12 carbon atoms, an optionally substituted aromatic radical having 6-12 carbon atoms or an optionally substituted araliphatic radical having 7-16 carbon atoms, which comprises reacting compounds of the formulae II or III see diagramm : EP0117448,P26,F2 in which n, R, R**1, R**2 and R**3 have the abovementioned meanings, with compounds of the formulae IV or V see diagramm : EP0117448,P26,F3 in which R, R**1, R**2, R**3 and n have the abovementioned meanings, if desired eliminating ester groups by hydrolysis or hydrogenolysis or if desired esterifying free carboxyl groups in a manner known per se.
申请公布号 JPS59172442(A) 申请公布日期 1984.09.29
申请号 JP19840015297 申请日期 1984.02.01
申请人 HOECHST AG 发明人 HANSUIERUKU URUBATSUHA;RAINERU HENINGU
分类号 A61K31/255;A61K31/40;A61K31/403;A61K31/404;A61P9/12;A61P43/00;C07C;C07C67/00;C07C215/00;C07C227/00;C07C227/14;C07C227/18;C07C229/02;C07C229/06;C07C229/16;C07C229/24;C07C229/26;C07C229/28;C07C229/36;C07C233/43;C07C253/00;C07C255/58;C07C271/06;C07C279/18;C07C301/00;C07C303/28;C07C309/03;C07C309/19;C07C309/63;C07C309/64;C07C309/65;C07C309/70;C07C313/00;C07C323/58;C07C325/00;C07C381/00;C07D207/323;C07D209/14;C07D209/18;C07D209/26;C07D209/44;C07D213/36;C07D217/12;C07D231/38;C07D233/88;C07D237/26;C07D239/26;C07D239/74;C07D241/36;C07D261/08;C07D263/32;C07D275/02;C07D277/58;C07D307/52;C07D307/81;C07D309/34;C07D317/48;C07D317/60;C07D333/20;C07D333/58;C07D401/12;C07D403/12;C07D405/12;C07D521/00;C07K5/06;C07K14/81 主分类号 A61K31/255
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