对氟肉桂酸置于4-二甲氨基吡啶,Lithium Aluminium Tetrahydride,Sodium Hydride,三乙胺体系中,用 四氢呋喃,二氯甲烷,二甲基亚砜,甲苯 用作溶剂,化学反应 2.33H,反应生成反式-4-(4-氟苯基)-3-羟甲基-1-甲基哌啶 参考文献:An Efficient And Stereoselective Synthesis Of (3S,4R)-(−)-Trans-4-(4'-Fluorophenyl)-3-Hydroxymethyl-N-Methylpiperidine 标题:An Efficient And Stereoselective Synthesis Of (3S,4R)-(−)-Trans-4-(4'-Fluorophenyl)-3-Hydroxymethyl-N-Methylpiperidine 摘要:An Asymmetric Conjugate Addition Reaction Between A Chiral Alpha,Beta-Unsaturated Amido Ester And Ethyl-N-Methylmalonamide Has Been Used As A Key Step In The Synthesis Of (3S,4R)-(-)-Trans-4-(4'-Fluorophenyl)-3-Hydroxymethyl-N-Methylpiperidine,A Key Intermediate For (-)-Paroxetine. (C) 2011 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Tetasy.2010.12.020
专利号:US-9315483-B2 优先权日:2007-09-13 标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof 发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT 权利人:CONCERT PHARMACEUTICALS INC 摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.
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-0037443-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 权利人:PENTECH PHARMACEUTICALS INC 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), where X is halogen, C1-C10 alkyl, C1-C10 alkoxy, C1-C10 haloalkyl, hydroxy, or hydrogen; and R2 and R3 each is C1-C4 alkyl and R2 and R3 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-2009035652-A1 优先权日:2007-09-13 标 题 :Synthesis of deuterated catechols and benzo[d][1,3] dioxoles and derivatives thereof
专利号:US-2014336387-A1 优先权日:2007-09-13 标题:Synthesis of deuterated catechols and benzo[d][1,3]dioxoles and derivatives thereof
专利号:EP-2200997-B9 优先权日:2007-09-13 标 题:Synthesis of deuterated benzodioxoles
1. Bao Z, Su B, Xing H, Yang Y, Ren Q. Enantioseparation of racemic paroxol on an amylose-based chiral stationary phase by supercritical fluid chromatography. J Sep Sci. 2010 Oct;33(20):3256-62. doi: 10.1002/jssc.201000422.