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2. 发明申请

WO0196282B1 METHOD FOR PRODUCING AMIDES OR ESTERS 审中-公开
标题翻译：用于生产酰胺或酯
公开(公告)号：WO0196282B1
公开(公告)日：2002-04-04
申请号：PCT/EP0106655
申请日：2001-06-12
申请人： DEGUSSA , GROEGER HARALD , SANS JUERGEN , BARTHUBER ANITA , HAINDL ROSWITHA
发明人： GROEGER HARALD , SANS JUERGEN , BARTHUBER ANITA , HAINDL ROSWITHA
IPC分类号： C07B61/00 , C07C67/08 , C07C69/76 , C07C231/02 , C07C233/05 , C07C233/65 , C07C269/06 , C07C271/22 , C07D251/46 , C07D487/08 , C07K1/08 , C07C69/78 , C07K1/10 , C07K5/06
CPC分类号： C07D487/08 , C07C67/08 , C07C231/02 , C07D251/46 , C07K1/084 , C07C233/05 , C07C233/65
摘要： The invention relates to a method for producing amides or esters from carboxylic acids and from an amine constituent or alcohol constituent in the presence of a 1,3,5-triazine and optionally in the presence of an organic solvent and of a tertiary amine. According to the invention, a (bi)cyclic diamine or an adduct formed therefrom with the triazine constituent is used as a tertiary amine in a preferred stoichiometric ratio of diamine to the triazine constituent ranging from 0.30 to 1.10; the stoichiometric ratio of carboxylic acid to the amine constituent or alcohol constituent should range from 0.2 to 5.0, and; the molar ratio of carboxylic acid to the triazine constituent ranges from 0.5 to 1.5. Amino acids such as N-protected amino acids and peptides serve as carboxylic acid constituents, and (C-protected) amino acids or a C-protected peptide serve as the amine constituent. 2-chlorine-4,6-dimethoxy-1,3,5-triazine (CDMT) is used as the preferred 1,3,5-triazine, and the N,N'-dimethyl-1,4-piperazine is used as the cyclic diamine. In addition to this method, which can be carried out at temperatures ranging from -80 to +150 DEG C and in the presence of an organic solvent, the invention also relates to adducts comprised of (bi)cyclic diamine and 1,3,5-triazine. Compared to the prior art, higher yields with shorter reaction times are achieved using the described method, and distinctly smaller waste quantities of tertiary amine bases accrue.
摘要翻译：本发明要求一种生产酰胺或选自羧酸酯和在1,3,5-三嗪的存在下和任选地在有机溶剂和叔胺的存在下，胺或醇成分，一种方法，其中所述叔胺的（双 - ）的环状二胺或具有从其中采用的优选的加合物的化学计量比为0.30的三嗪组分1.10三嗪组分形成; 羧酸的化学计量比与胺或醇组分应为0.2和5.0之间，和羧酸的摩尔比三嗪0.5〜1.5。作为羧酸成分，如氨基酸发生 N-保护的氨基酸和肽和作为胺组分（C保护的）氨基酸或有问题的C保护的肽。作为优选的1,3,5-三嗪，2-氯-4,6-二甲氧基-1,3,5-三嗪（CDMT），并用于N'-二甲基-1,4-哌嗪作为环状二胺N. 除了这种方法，可以在-80和+ 150℃之间的温度下进行，并在有机溶剂的存在下，本发明还要求（二环）环二胺和1,3,5-三嗪的加成物。用本发明的方法，在较短的反应时间相比于现有技术和有显著在叔胺碱较低量的废物获得更高的产量。

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