专利号:WO-2015071831-A1 优先权日:2013-11-18 标 题 :An improved process for minimising the formation of dehalogenated byproducts 发明人:KADAM SHASHIKANT; ARADDY RAJSHEKAR; KONDRAGUNTA VENKATESWARA RAO; HULAVALE YOGESH; SOMISETTI NARENDER RAO; CHENNAMSETTY SUNEEL MANOHAR BABU; HARIHARAN SIVARAMAKRISHNAN 权利人:PIRAMAL ENTPR LTD 摘要:The present invention provides an improved process for preparation of organic compounds represented by Formula-Z; wherein effectively minimising the formation of dehalogenated by-products is achieved. In the process, the reduction is carried out using suitable reducing agent; more preferably Lithium Aluminium Hydride (LAH) in a solvent system, wherein at least one of the solvent is selected from halogenated solvents, which acts as co-solvent. The process of the present invention is useful for minimising of the formation of dehalogenated by-products during synthesis of various active pharmaceutical ingredients such as Paroxetine Hydrochloride, Cinacalcet, Eletriptan and Asenapine.
专利号:US-2001053862-A1 优先权日:1998-12-22 标 题:Process for preparing arylpiperidine carbinol intermediates and derivatives 发明人:RONSEN BRUCE; UPADHYAYA SUBHASH P 摘要:A process for the synthesis of arylpiperidine carbinol intermediates and derivatives is disclosed. A preferred process embodiment provides the synthesis of intermediate compounds of structural formula (I) and structural formula (II): n n n where X is halo, C 1 -C 10 alkoxy, C 1 -C 10 haloalkyl, or hydroxy; R 2 and R 3 are each C 1 -C 4 alkyl, and R 2 and R 3 are the same. The compound of structural formula (I) is made by condensing a corresponding cinnamonitrile with a corresponding diester malonate. The compound of structural formula (II) in the (±)-trans configuration is obtained by hydrogenating the compound of structural formula (I). The compounds of structural formula (I) and structural formula (II) are useful chemical intermediates for synthesizing 4-arylpiperidine-3-carbinols and their derivatives in (−)-trans configuration.
专利号:WO-2009005647-A2 优先权日:2007-06-27 标 题 :Compounds and process to prepare chiral intermediates for synthesis of paroxetine
参考标题:Catalytic Michael/ring-Closure Reaction Of α,β-Unsaturated Pyrazoleamides With Amidomalonates: Asymmetric Synthesis Of (−)-Paroxetine 作者:Yu Zhang,Yuting Liao,Xiaohua Liu,Qian Yao,Yuhang Zhou,Lili Lin,Xiaoming Feng |发布日期:2016.10.10 摘要:A Highly Enantioselective Tandem Michael/ring‐closure Reaction Of α,β‐unsaturated Pyrazoleamides And Amidomalonates Has Been Accomplished In The Presence Of A Chiral N,N′‐dioxide-Yb(Otf)3 Complex (Tf: Trifluoromethanesulfonyl) To Give Various Substituted Chiral Glutarimides With High Yields And Diastereo‐ And Enantioselectivities. Moreover, This Methodology Could Be Used For Gram‐scale Manipulation