专利号:US-8779121-B2 优先权日:2012-10-12 标题:Process for the synthesis of 3-(2-bromo-4,5-dimethoxyphenyl)propanenitrile, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 发明人:CARRANZA MARIA DEL PILAR; GARCIA ARANDA MARIA ISABEL; GONZALEZ JOSÉ LORENZO; SANCHEZ FRÉDÉRIC 权利人:SERVIER LAB 摘要:Process for the synthesis of the compound of formula (I): n nApplication in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
专利号:US-9090742-B2 优先权日:2013-06-28 标 题 :Facile synthesis of metalloporphyrin polymers 发明人:VAIL SEAN; EVANS DAVID 权利人:SHARP LAB OF AMERICA INC 摘要:A method is provided for synthesizing a metal (M) meso-tetraphenylporphyrin polymer. The method begins with the provision of a free-base (H 2 )-meso-tetra-4-(trialkylsilyl)ethynylphenylporphyrin (H 2 -tetra-C≡C-TriAS-TPP) including a trialkylsilyl (TriAS) moiety attached to an ethynyl termini. In response to a reaction with a metal (M)-containing material, the H 2 -tetra-C≡C-TriAS-TPP is converted to a metal (M)-tetra-4-(trialkylsilyl)ethynylphenylporphyrin (M-tetra-C≡C-TriAS-TPP). Then, the M-tetra-C≡C-TriAS-TPP is converted to a M-tetra-4-ethynylphenylporphyrin (M-tetra-C≡C-TPP) monomer by removing the trialkylsilyl (TriAS) moiety from the ethynyl termini. Finally, a plurality of M-tetra-C≡C-TPP monomers are coupled together to supply a metal (M)-meso-tetraphenylporphyrin polymer (M-poly-meso-TPP), whereby meso-phenyl groups of adjacent M-tetra-C≡C-TPP monomers in the M-poly-meso-TPP are connected through a butadiyne linking moiety. In one aspect, the metal is zinc.
专利号:US-6448058-B1 优先权日:1997-09-12 标 题:Methods for solid phase synthesis of mercapto compounds and derivatives, combinatorial libraries thereof and compositions obtained thereby 发明人:PATEL DINESH V; NGU KHEHYONG; ZHOU JIANPING 权利人:VERSICOR INC 摘要:Methods of preparing combinatorial libraries of mercapto (thiol) compounds them and compositions obtained therefrom are disclosed. The compounds are synthesized on a solid support. Following synthesis, the compounds are optionally cleaved from the support. One such method of synthesis involves attack of an S-protected nucleophile on a resin functionalized with a leaving group. The invention also provides for screening the mercapto compounds for bioactive compounds; in particular, for inhibitors of MMPs.
专利号:US-5756790-A 优先权日:1995-09-29 标题 :Optically active cobalt (II) complexes and method for the preparation of optically active alcohols 发明人:MUKAIYAMA TERUAKI; YOROZU KIYOTAKA; NAGATA TAKUSHI; YAMADA TORU; SUGI KIYOAKI 权利人:MITSUI PETROCHEMICAL IND 摘要:The invention provides a method for preparing an optically active alcohol comprising the step of reacting a ketone compound with a hydride reagent in the presence of an optically active metal compound. The resulting optically active alcohols are useful as intermediates for the synthesis of physiologically active compounds such as drugs and pesticides, functional materials such as liquid crystals, and raw materials for synthesis in fine chemistry. A novel optically active cobalt (II) complex useful as a catalyst is also provided.
专利号:WO-0026190-A1 优先权日:1998-10-30 标 题:Chiral amino alcohol derivatives of pyridine, a method for the manufacture thereof and their use as catalysts 发明人:NEVALAINEN VESA; SYLVESTRE DEGNI 权利人:NESTE CHEMICALS OY; NEVALAINEN VESA; SYLVESTRE DEGNI 摘要:The invention relates to chiral amino alcohol derivatives of pyridine, which compounds are useful as catalysts in combination with organic zinc compounds for asymmetric induction reactions and more particularly for enantioselective synthesis of optically active alcohols from aldehydes. The invention also relates to a process for the preparation of the said amino alcohol derivatives of pyridine and to a method for the manufacture of optically active alcohols from aldehydes in the presence of organic zinc compounds and amino alcohol derivatives of pyridine.
专利号:US-10017474-B1 优先权日:2018-01-02 标题 :Method of synthesizing (E)-1,2-di(pyridin-2-yl) ethene-1,2-diol 发明人:AL-ZEQRI NABIL AHMED QASSIM; WARAD ISMAIL KHALIL; AWWADI FIRAS FANDI; ALSALME ALI MOHAMMED; ALALI ANAS KHALED ABED; ZARROUK ABDELKADER 权利人:UNIV KING SAUD 摘要:The method of synthesizing (E)-1,2-di(pyridine-2-yl)ethene-1,2-diol involves dimerization of 2-pyridinecarboxaldehyde (also referred to herein as “picolinaldehydeâ€?). The synthesis of the desired ethene-1,2-diol is achieved using a Cu(II) catalyst to dimerize picolinaldehyde under mild conditions. Preferably, the Cu(II) catalyst is a Cu(II)/neocuproine (2,9-dimethyl-1,10-phenanthroline) complex, or other Cu(II)/phen complex. The reaction in this embodiment may occur at room atmosphere and in ambient light conditions using a water/ROH solvent. The exemplary ethene-1,2-diol product, (E)-1,2-di(pyridin-2-yl)ethene-1,2-diol has the following structural formula:
[参考文献]: Kim Ds, Et Al. Hydroesterification Of Alkenes With Sodium Formate And Alcohols Promoted By Cooperative Catalysis Of Ru3(Co)12 And 2-Pyridinemethanol. J Org Chem. 2014 Dec 19;79(24):12191-6. [参考文献]: Masazumi Tamura, Et Al. Self-Assembled Hybrid Metal Oxide Base Catalysts Prepared By Simply Mixing With Organic Modifiers. Nat Commun. 2015 Oct 5:6:8580.
合成参考文献
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