CAS: 26447-85-8; Methyl 2-Hydroxy-2,2-Di(Thiophen-2-yl)Acetate

上下游产品

Dimethyl oxalate acetic acid thiophen-2-yl magnesium bromide 2-bromothiophene(1R,3S,5S)-2'-hydroxy-2',2'-di(thiophen-2''-yl)acetic acid 8-methyl-8-azabicyclo[3.2.1]°Ct-6-en-3-yl ester N-demethyltiotropium hydroxydithien-2-ylacetic acid 1-aza-bicyclo[2.2.2]°Ct-3(R)-yl ester 2-hydroxy-2,2-dithien-2-ylacetic acid (3R)-1-(2-phenoxyethyl)pyrrolidin-3-yl ester

草酸二甲酯置于magnesium,硫酸体系中,用 乙醚 用作溶剂,化学反应 4.75H,以60%的收率获得2,2-二噻吩基乙醇酸甲酯
参考文献:Azabicycloalkane Compounds
标题:Azabicycloalkane Compounds
摘要:这项发明提供了式i的化合物: 其中r1,R2,R3,R4,R5,R6和r7如规范中所定义,或其药用可接受盐,溶剂或立体异构体.本发明的化合物具有β2肾上腺素受体激动剂和肌碱受体拮抗剂活性.这些化合物对治疗肺部疾病,如慢性阻塞性肺病和哮喘,是有用的.

专利信息

专利号:WO-2018154596-A1
优先权日:2017-02-22
标 题 :Process for synthesis of tiotropium bromide monohydrate
发明人：REDDY G NITHUN; REDDY G SAMHITHA; REDDY G MADAALASA; RAMANI M; REDDY G PRATAP
权利人:GBR LABORATORIES PVT LTD; RACHANA PHARMA TECH
摘要:Provided herein is a process for synthesis of tiotropium bromide wherein the coupling of scopine with 2, 2-dithienyl glycolate is achieved by a two step process under mild conditions.

专利号:WO-2013046138-A1
优先权日:2011-09-27
标 题:Process for the preparation of scopine esters
发明人：CIPOLLONE AMALIA; FATTORI DANIELA; FINCHAM CHRISTOFER INGO
权利人:LUSOCHIMICA SPA
摘要:The present invention relates to a process for the preparation of scopine esters, as intermediates in the synthesis of tiotropium bromide. In particular, it relates to a transesterification process between scopine alcohol and an ester of a carboxyl acid in high yields and under conditions suitable for industrial use.

专利号:WO-2021133280-A1
优先权日:2019-12-27
标 题 :An improved process for preparation of scopine hydrobromide
发明人：HAAS PHILIPP DANIEL; STECKEL HARTWIG ANDREAS; BELLUR ATICI ESEN; AYDIN FATMA GÖZDE
权利人:DEVA HOLDING
摘要:The present invention relates to an efficient and industrially advantageous process for the preparation of scopine free base or salts. Said compounds are important intermediates in the synthesis of tiotropium and pharmaceutically acceptable salts thereof. The method provided for preparing scopine free base or its salts has the advantages of a simple operation, high yield and low costs.

专利号:US-8680297-B2
优先权日:2011-10-06
标 题 :Manufacturing process for tiotropium bromide
发明人：SOUKUP MILAN
权利人:SOUKUP MILAN; DRUG PROCESS LICENSING ASSOC LLC
摘要:The present invention relates to a novel manufacturing process of pharmaceutically active compound of formula I used as a long-acting anticholinergic bronchodilator. Starting from oxalic acid derivative of formula III the invention describes preparation of a novel cyclic anhydride of formula II which is very efficient precursor in the synthesis of Tiotropium bromide (compound of formula I).

专利号:US-9440945-B2
优先权日:2010-04-01
标 题 :Methods for the synthesis of tiotropium bromide
发明人：BILGIC MAHMUT
权利人:BILGIC MAHMUT
摘要:Present invention relates to methods for preparing (1α, 2β, 4β, 5α, 7β)-7-[(hydroxidi-2-thienllacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.0 2,4 ]nonane-bromide.

专利号:EP-2825535-B1
优先权日:2012-03-16
标 题 :A method of preparing the scopine ester of di-(2-thienyl)glycolic acid, an intermediate in the synthesis of tiotropium bromide, and its new form
发明人：CERNA IGOR; HAJICEK JOSEF
权利人:ZENTIVA KS