METHOD FOR PREPARING SITAGLIPTIN INTERMEDIATE VIA ASYMMETRICAL REDUCTION METHOD

Title:

METHOD FOR PREPARING SITAGLIPTIN INTERMEDIATE VIA ASYMMETRICAL REDUCTION METHOD

Document Type and Number:

WIPO Patent Application WO/2016/055015

Kind Code:

A1

Abstract:

Disclosed is a method for synthesizing a sitagliptin intermediate, the method comprising: under the existence of transition metal catalyst of chiral phosphine ligand and hydrogen, conducting asymmetrical reduction ammonification reaction on a formula II compound and ammonia salt or ammonium salt in a proper organic solvent under the condition of adding an acidic additive, and obtaining a formula I compound, wherein, a configuration of R- or S- of a stereocenter is represented by *; the formula I compound of R configuration can be used to prepare sitagliptin, and a reaction formula is as the following: R1 and R2 are respectively and independently selected from hydrogen, C1-C12 straight chain or branched-chain alkyl, C3-C12 cycloalkyl, C2-C12 chain alkenyl, C2-C12 chain alkynyl and C7-C12 arylalkyl. The method has a high yield and a high ee% value, a mild reaction condition and a low production cost, is simple to operate and convenient to purify, and is environmentally friendly and suitable for industrial production.

Inventors:

HONG JIAN (CN)
WANG YUSHENG (CN)
WANG BOYU (CN)
HUANG LUNING (CN)
GU ERIC (CN)

Application Number:

PCT/CN2015/091539

Publication Date:

April 14, 2016

Filing Date:

October 09, 2015

Export Citation:

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Assignee:

ZHEJIANG HUAHAI PHARM CO LTD (CN)
SHANGHAI SYNCORES TECHNOLOGIES INC LTD (CN)

International Classes:

C07C227/32; C07C229/34; C07C269/04; C07C271/22

Foreign References:

CN102702205A	2012-10-03
CN103755596A	2014-04-30

Other References: