专利号:US-7825244-B2 优先权日:2005-06-10 标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis 发明人:BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG 权利人:JANSSEN PHARMACEUTICA NV 摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.
专利号:US-12202783-B2 优先权日:2019-04-02 标题 :Method for synthesis of organic iodides, a perovskite-forming composition comprising an organic iodide and a photovoltaic cell with a perovskite layer obtained therefrom 发明人:MISZTAL KASJAN; WOJCIECHOWSKI KONRAD; MALINKIEWICZ OLGA; MIARA ZBIGNIEW 权利人:SAULE S A 摘要:A method for obtaining a salt with a general formula: RxNI, wherein: RxN is an organic cation (RxN+), R represents substituents (R—) independently selected from a group consisting of organic substituents: R1—, R2—, R3— and hydrogen (H—), x is a number of the substituents R— directly linked with the nitrogen (N) atom in the organic cation RxN+, wherein x is 3 or 4, I is an iodide anion (I−). The method comprises: preparing a reaction mixture comprising the steps of: synthesizing hydrogen iodide (HI) in situ by mixing molecular iodine (I2) with formic acid (COOH) in a molar ratio of molecular iodine (I2): formic acid (COOH) of no less than 1.01:1, in a solvent medium, introducing into the solvent medium a compound being a donor of organic cation RxN+ in an amount providing the molar ratio of the donor of organic cation RxN+: molecular iodine (I2) of no less than 1.01:1, and maintaining the reaction mixture at a temperature of not less than 20° C. for the time necessary to obtain the reaction product being the salt with the general formula RxNI. The obtained product is a substrate for synthesis of perovskites.
专利号:US-11999749-B2 优先权日:2021-06-30 标题 :Synthesis of a bis-mesylate salt of 4-amino-N-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide and intermediates thereto 发明人:GOSSELIN FRANCIS; KOENIG STEFAN G; MERCADO-MARIN EDUARDO V; STUMPF ANDREAS; ZELL DANIEL; ZHANG HAIMING; BACHMANN STEPHAN; CARRERA DIANE E; DALZIEL MICHAEL E; GE YONGHUI; ZHANG JIE; BIGLER RAPHAEL; FINET LAURE ELIZABETH SIMONE; MONDIERE REGIS JEAN GEORGES; NAKAGAWA YUKI 权利人:GENENTECH INC; HOFFMANN LA ROCHE 摘要:A manufacturing process to a bis-mesylate salt 1b of the pan-RAF inhibitor 4-amino-n-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide. The process features a number of efficient key reactions, including a robust and scalable Pd-catalyzed carbonylation reaction to generate thienopyrimidine 2 and a highly chemoselective Pt/V/C-catalyzed nitro group reduction to access penultimate intermediate 7. The final amide coupling of 7 and 2 was accomplished by a mild and safe protocol employing N,N,N′,N′-tetramethylchloroformamidinium hexafluorophosphate (TCFH) as the coupling reagent, to produce a 1:1 adduct of the freebase and THF. The adduct afforded compound 1b with excellent yield, purity, and form stability on a multikilogram production scale after reaction with MsOH and recrystallization. The methods are able to produce a compound having upwards of 95% purity.
专利号:US-10053420-B2 优先权日:2015-01-30 标 题 :Processes for the preparation of compounds, such as 3-arylbutanals, useful in the synthesis of medetomidine 发明人:EKLUND LARS; EEK MARGUS; EKAMBARAM RAMESH; MAASALU ANTS 权利人:CAMBREX KARLSKOGA AB 摘要:There is provided a process for the preparation of a compound of formula (I) as defined herein, wherein said process comprises reacting a compound of formula (II) as defined s herein with one or more suitable Vilsmeier reagent.
专利号:US-9278939-B2 优先权日:2013-09-18 标 题:Methods for preparation of (4,6-dihalo-pyrimidin-5-yl)-acetaldehydes 发明人:LU SHAOPO; LI ZHUOCAI 权利人:SUZHOU JONATHAN NEW MATERIAL TECHNOLOGY CO LTD 摘要:This invention relates to the synthesis of chemical compounds and particularly to methods for the preparation of (4,6-dihalo-pyrimidin-5-yl)-acetaldehydes. The methods involve preparing a compound of the following general formula V from a compound of the following general formula IV through hydrolysis under the action of mercury dichloride and calcium carbonate, according to the following equation: n nwherein X is Cl or Br. The methods offer the benefits of use of highly available materials, high step yields, moderate reaction conditions, simply post-processing and purification, and suitability to industrialized production.
专利号:US-8993753-B2 优先权日:2009-08-06 标题:Stereoselective synthesis of bicyclic heterocycles 发明人:OSTERMEIER MARKUS; DAEUBLER JUERGEN; HUCHLER GUENTHER; KLING STEPHAN; SANTAGOSTINO MARCO 权利人:OSTERMEIER MARKUS; DAEUBLER JUERGEN; HUCHLER GUENTHER; KLING STEPHAN; SANTAGOSTINO MARCO; BOEHRINGER INGELHEIM INT 摘要:The present invention relates to a process for the stereoselective preparation of compounds of formulae (1A) and (1B) n nand the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways.