专利号:US-10711138-B2 优先权日:2016-04-08 标题:Intermediates and procedures for the synthesis of functional materials 发明人:KIRSCH PEER; GUNST SUSANN 权利人:MERCK PATENT GMBH 摘要:The present invention relates to heteroaromatic compounds which have two different reactive groups, their use in the synthesis of asymmetrically substituted compounds, and synthesis processes in which the compounds according to the invention are reacted sequentially with two different compounds, whereby an asymmetrically substituted compound is formed.
专利号:US-8877930-B2 优先权日:2009-11-04 标 题 :Continuous flow synthesis of amino alcohols using microreactors 发明人:BEDORE MATTHEW W; ZABORENKO NIKOLAY; JENSEN KLAVS F; JAMISON TIMOTHY F 权利人:BEDORE MATTHEW W; ZABORENKO NIKOLAY; JENSEN KLAVS F; JAMISON TIMOTHY F; MASSACHUSETTS INST TECHNOLOGY 摘要:The present invention provides various methods for the synthesis of chemical species in a microreactor environment. In some cases, reaction products of the present invention may be valuable as intermediates and/or products in pharmaceutical and polymer research. For example, the method may involve the synthesis of amino alcohols within a microchannel. Embodiment described herein may allow for reactions with significantly shorter reaction times and increased efficiency.
专利号:US-8735586-B2 优先权日:2007-06-26 标 题 :Regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR 权利人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR; SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct copper catalyzed regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
专利号:EP-2173747-B1 优先权日:2007-06-26 标 题:A regioselective metal catalyzed synthesis of annelated benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; R KYEN OMAR; URMANN MATHIAS; HALLAND NIS 权利人:SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
专利号:US-8729310-B2 优先权日:2009-09-22 标题:Halogenated diarylamine compound and synthesis method thereof 发明人:OSAKA HARUE; INOUE HIROTO 权利人:OSAKA HARUE; INOUE HIROTO; SEMICONDUCTOR ENERGY LAB 摘要:An object is to provide a new halogenated diarylamine compound serving as a source material for synthesis of a variety of diarylamine compounds and triarylamine compounds and a synthesis method of the new halogenated diarylamine compound. A halogenated diarylamine compound represented by the following general formula (G1) and a synthesis method thereof are provided. Note that a variety of diarylamine compounds and triarylamine compounds can be synthesized using the halogenated diarylamine compound represented by the following general formula (G1).
专利号:US-8735391-B2 优先权日:2008-09-26 标 题 :Synthesis of functionalized octahydro-isoquinolin-1-one-8-carboxamides, octahydro-isoquinolin-1-one-8-carboxylic esters and analogs, and therapeutic methods 发明人:AUBE JEFFREY; ROTH BRYAN L; GHOSH PARTHA; FRANKOWSKI KEVIN J 权利人:AUBE JEFFREY; ROTH BRYAN L; GHOSH PARTHA; FRANKOWSKI KEVIN J; UNIV KANSAS 摘要:A functionalized polycyclic compound can have a structure of Formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined Diels-Alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of Formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor. Such opioid modulation can provide a biological benefit to a subject.
[参考文献]: E C Riesgo, Et Al. Crowded Cu(I) Complexes Involving Benzo[参考文献]: E J Lavoie, Et Al. Identification Of The Metabolites Of Benzo[参考文献]: E J Lavoie, Et Al. The Carcinogenicity Of Quinoline And Benzoquinolines In Newborn Cd-1 Mice. Jpn J Cancer Res. 1987 Feb;78(2):139-43. [参考文献]: Halehatty R Prakash Naik, Et Al. Synthesis Of Novel Benzo[参考文献]: John B Sutherland, Et Al. Fungal Biotransformation Of Benzo[f]Quinoline, Benzo[h]Quinoline, And Phenanthridine. Appl Microbiol Biotechnol. 2005 May;67(3):405-11.