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Patent
Zhejiang Jiuzhou Pharmaceutical Co. | Date: 2014-06-23

The present invention relates to the field of medical synthesis, in particular to a preparation method for pyrrolidine-2-carboxylic acid derivatives. The present invention adopts the following technical solution: providing a compound having a structure of formula (E), wherein R is R_(1 )or R_(2), R_(1 )is C_(1)-C_(6 )an alkyl, benzyl, p-methoxybenzyl, or p-nitrobenzyl group, and R_(2 )is hydrogen; R_(3 )is a protecting group of the carboxyl group; and P_(1 )is a protecting group on nitrogen.


Patent
Zhejiang Jiuzhou Pharmaceutical Co. | Date: 2016-05-04

The present invention relates to the field of medical synthesis, in particular to a preparation method for pyrrolidine-2-carboxylic acid derivatives. The present invention adopts the following technical solution: providing a compound having a structure of formula (E), wherein R is R_(1) or R2, R1 is C1-C6 an alkyl, benzyl, p-methoxybenzyl, or p-nitrobenzyl group, and R2 is hydrogen; R3 is a protecting group of the carboxyl group; and P1 is a protecting group on nitrogen.


Patent
Zhejiang Jiuzhou Pharmaceutical Co. | Date: 2012-08-01

The present invention relates to Sitagliptin intermediate and preparation method and use thereof. The method comprises reacting compound of formula (II) and trifluorobromobenzene with a Grignard reagent by a Grignard reaction to obtain a compound of formula (I). Compound of formula (I) is a new intermediate compound for the synthesis of Sitagliptin. Compound of formula (I) can be easily used for preparing another important intermediate compound of formula (V) for the synthesis of Sitagliptin. The structures of the compounds mentioned above are as the following:


Patent
Zhejiang Jiuzhou Pharmaceutical Co. | Date: 2012-07-27

The present invention relates to a spirobenzylamine-phosphine, preparation method therefor and use thereof. The compound has a structure represented by formula (I), wherein n=0 to 3; R^(1), R^(2), R^(3), R^(4), R^(5), R^(6), R^(7), R^(8 )and R^(9 )having a value as defined in claim 1. Starting from the substituted 7-trifluoromesyloxy-7-diarylphosphino-1,1-spiro-dihydroindene, the compound is synthesized in a two-step or three-step reactions. The new spirobenzylamine-phosphine is complexed with an iridium precursor and is subjected to ion exchange, to give an Iridium/spirobenzylamine-phosphine complex comprising various anions. The spiro benzyl amine-phosphine/Iridium complex according to the present invention may be used for catalyzing asymmetry hydrogenation of a variety of alpha-substituted acrylic acids, has high activity and enantio-selectivity, and has a good prospect of industrialization.


Patent
Zhejiang Jiuzhou Pharmaceutical Co. | Date: 2013-01-30

The invention relates to Sitagliptin intermediate compounds of formula (f), preparation methods and uses thereof. The compound of formula (f) are prepared by the following steps: compounds of formula (a) are subjected to electrophilic reaction with benzyl halides to form compounds of formula (b), which then react with compounds of formula (i) to form novel compounds of formula (e); Gignard agents formed from 2,4,5-trifluoro bromobenzene and magnesium metal react with compounds of formula (e) to afford compounds of formula (f), which are novel intermediate compounds for the preparation of Sitagliptin intermediates of formula (g). The compound of formula (f) was subjected to reduction by Pd/C, debenzylation, substitution of protecting group to form the compounds of formula (g). The mentioned compounds have the following structures, wherein, R is the protecting group of carboxyl, R^(2) is (substituted) hydrocarbyl.


Patent
Zhejiang Jiuzhou Pharmaceutical Co. | Date: 2014-07-09

The present invention relates to a spirobenzylamine-phosphine, preparation method therefor and use thereof. The compound has a structure represented by formula (I), wherein n=0 to 3; R^(1), R^(2), R^(3), R^(4), R^(5), R^(6), R^(7), R^(8) and R^(9) having a value as defined in claim 1. Starting from the substituted 7-trifluoromesyloxy-7-diarylphosphino-1, 1-spiro-dihydroindene, the compound is synthesized in a two-step or three-step reactions. The new spirobenzylamine-phosphine is complexed with an iridium precursor and is subjected to ion exchange, to give an Iridium/spirobenzylamine-phosphine complex comprising various anions. The spiro benzyl amine-phosphine/Iridium complex according to the present invention may be used for catalyzing asymmetry hydrogenation of a variety of alpha-substituted acrylic acids, has high activity and enantio-selectivity, and has a good prospect of industrialization.


Patent
Zhejiang Jiuzhou Pharmaceutical Co. | Date: 2012-06-29

A new compound is provided, which is used for preparing lacosamide. A novel method for preparing lacosamide is also provided. During the reaction, iodomethane and silver oxide that are cost expensive are not used, nor a Pd-c catalyst is used, so the production cost is low, the raw materials and accessory materials are cheap and easily available, and the process is simple, so that industrial production is easy to realize; and moreover, the yield is high, and good economic efficiency can be achieved.


Patent
Zhejiang Jiuzhou Pharmaceutical Co. | Date: 2014-11-12

Disclosed are a silodosin intermediate and a preparation method thereof. The silodosin intermediate has the structure shown by the formula (A). X is hydrogen or bromide and R^(1) is hydrogen. The formyl group may be a group having the structure shown by the formula I. R^(7) is an carboxyl-protecting group, and R^(2) is 3-hydroxypropyl or a group having the structure shown by the formula II. W is a hydroxyl-protecting group. A compound of the formula (A) according to the present invention may further be used for preparing a compound having the structure shown by the formula (D). By means of the intermediate and the preparation method therefor provided by the present invention, high-purity optically pure silodosin can be obtained, and the optical purity is above 99%.


Patent
Zhejiang Jiuzhou Pharmaceutical Co. | Date: 2014-02-13

The present invention relates to the technical field of medicine and organic synthesis, particularly to a method for preparing crizotinib. The method comprises the compound of formula b and the compound of formula e undergoing Suzuki coupling reaction to produce the compound of formula a which then was subjected to deprotection to afford () crizotinib.


Patent
Zhejiang Jiuzhou Pharmaceutical Co. | Date: 2013-09-02

The invention relates to a new enantioselective process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a -amino--biphenyl--methylalkanoic acid, or acid ester, backbone.

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