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1.发明公开METHOD FOR PREPARING PYRAZOLECARBOXYLIC ACID DERIVATIVE, AND INTERMEDIATE THEREOF 审中-公开制备吡唑羧酸衍生物的方法及其中间体
公开(公告)号：EP3312161A1
公开(公告)日：2018-04-25
申请号：EP16810995.7
申请日：2016-06-15
发明人： SHAO, Hongming , HE, Renbao , JIN, Yizhong , WANG, Lei
IPC分类号： C07D231/12 , C07D231/14 , C07D251/30 , C07C221/00 , C07C225/14 , C07C49/255 , C07D295/125
摘要： Provided are a preparation method for synthesizing a pyrazolecarboxylic acid derivative of the following formula (I), which is suitable for industrial production, and an intermediate as shown by the following formula (II). The method is high in reaction yield in each step, low in waste gas and waste water and low in cost, and requires no special reaction equipment.
摘要翻译： 本发明提供适于工业生产的下式（I）的吡唑羧酸衍生物和下式（II）所示的中间体的合成方法。 该方法每步反应收率高，废气和废水量少，成本低，不需要特殊的反应设备。
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公开(公告)号：EP3312161B1
公开(公告)日：2020-11-04
申请号：EP16810995.7
申请日：2016-06-15
发明人： SHAO, Hongming , HE, Renbao , JIN, Yizhong , WANG, Lei
IPC分类号： C07D231/12 , C07D231/14 , C07D251/30 , C07C221/00 , C07C225/14 , C07C49/255 , C07D295/125
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公开(公告)号：EP4050102A1
公开(公告)日：2022-08-31
申请号：EP21884273.0
申请日：2021-01-21
申请人： Zhejiang Yongtai Technology Co., Ltd. , Zhejiang University of Technology , Zhejiang Yongtai Pharmaceutical Co., Ltd.
发明人： LIU, Zhiqiang , CHENG, Feng , ZHANG, Xiaojian , JIA, Dongxu , ZHENG, Yuguo , HE, Renbao , JIN, Yizhong , SHAO, Hongming , LIN, Jiaohua , ZHANG, Feng
摘要： The present invention discloses a transaminase mutant and application thereof in preparation of sitagliptin intermediates, the transaminase mutant is obtained by substitution of tyrosine with proline at position 74, substitution of glutamic acid with aspartic acid at position 228, substitution of leucine with alanine at position 254 and substitution of methionine with threonine at position 290 of the amino acid sequence shown in SEQ ID NO: 2. The present invention uses wet cells or a purified transaminase as a biocatalyst and a sitagliptin precursor ketone or a prochiral carbonyl compound as a substrate to prepare a sitagliptin intermediate or a sitagliptin ester intermediate; the total yield of the method reaches about 82%, and e.e. value of the product reaches 99%.
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4.发明公开
公开(公告)号：EP3498695A1
公开(公告)日：2019-06-19
申请号：EP16913341.0
申请日：2016-09-29
发明人： HE, Renbao , WANG, Yingshu , SHAO, Hongming , JIN, Yizhong
IPC分类号： C07D231/14
摘要： The present invention relates to a method for synthesizing a compound of 3-(difluoromethyl)-1-methyl-1h-pyrazole-4-carboxylic acid, wherein including the steps of:
(A) the diethyl ester compounds represented by the following Formula IV are reacted under the action of amine, alkali and carbonyl reagents to produce the acrylic diester compound represented by the following Formula I,
wherein :
R 1 =
R 2 =
(B) the above compound represented by the Formula I is reacted with a fluoride reagent, a Lewis acid and a methyl hydrazine to form a pyrazole ring-containing diester compound represented by the Formula II,
(C) the heterocyclic-containing diester compound represented by the Formula II is reacted with a base to give 3-(difluoromethyl)-1-methyl-1h-pyrazole-4-carboxylic acid represented by the Formula III.
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