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Title:
PROCESS FOR MILD ESTERIFICATION OF A CARBOXYLIC ACID WITH AN ALCOHOL COMPONENT
Document Type and Number:
Japanese Patent JPH03184924
Kind Code:
A
Abstract:

PURPOSE: To esterify an α-amino-protected amino acid, by esterfying an α-amino- suitably protected amino acid in an aprotic and non-basic solvent in the presence of 2,4,6-mesitylene-1-sulfonyl-3-nitro-1,2,4-triazolide and a weak base.

CONSTITUTION: In the esterification of a protected amino acid, especially α- amino-protected amino acid, with an alcohol component in the presence of 2,4,6-mesitylene-1-sulfonyl-3-nitro-1,2,4-triazolide(MSNT) and a weak base, the esterification is effected in an aprotic and non-basic solvent (e.g. dichloromethane, THF) in the presence of N-methylimidazole(MeIm) under mild conditions. Preferred molar ratio of amino acid:MSTN:MeIm is 1:1:1 or less (especially 0.75) or less. As the alcohol component are used low molecular components such as protecting groups, polymer components such as soluble carriers or solid carriers.


Inventors:
BIRUGITO BURANKEMAIYAAAMENGE
RONARUDO FURANKU
Application Number:
JP22787890A
Publication Date:
August 12, 1991
Filing Date:
August 29, 1990
Export Citation:
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Assignee:
BIOTECHNOLOG FORSCHUNG GMBH
International Classes:
C07B41/12; C07C67/08; C07C227/18; C07C227/32; C07C269/06; C08B3/14; C08F8/14; (IPC1-7): C07B41/12; C07C227/18; C07C227/32
Attorney, Agent or Firm:
Kiyoya Fujino (1 outside)