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📜叔-丁基氯甲酸酯置于4-二甲氨基吡啶,三乙胺体系中,用 二氯甲烷 用作溶剂,化学反应生成1-Boc-4-甲烷磺酰氧基哌啶
参考文献:一种克里唑替尼中间体制备方法
标题:一种克里唑替尼中间体制备方法
摘要:本发明为抗肿瘤分子靶向药物克里唑替尼的合成方法,属于制药领域.涉及一种克里唑替尼中间体的合成方法,包括两种还原工艺,一种溴代反应工艺,反应步骤如下:还原工艺一:化合物(R)‑3‑[1‑(2,6‑二氯‑3‑氟苯基)乙氧基]‑2‑硝基吡啶与连二硫酸钠,在机械化学条件下发生还原反应,生成(R)‑3‑[1‑(2,6‑二氯‑3‑氟苯基)乙氧基]‑2‑氨基吡啶;还原工艺二:化合物(R)‑3‑[1‑(2,6‑二氯‑3‑氟苯基)乙氧基]‑2‑硝基吡啶溶于有机溶剂中,催化加氢,还原生成(R)‑3‑[1‑(2,6‑二氯‑3‑氟苯基)乙氧基]‑2‑氨基吡啶;溴代反应工艺:将上述化合物与过硫酸氢钾和溴化盐反应,得到克里唑替尼中间体.该工艺成本低,原材料易购买,操作简便安全,收率高,适用于大规模生产.

专利信息

专利号:US-2010004245-A1
优先权日:2006-10-20
标 题:Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：OBALLA RENATA M; DESCHENES DENIS; GAGNON MARC; LEBLANC YVES; POWELL DAVID; RAMTOHUL YEEMAN K
权利人:MERCK FROSST CANADA LTD
摘要:Azacycloalkane derivatives of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.

专利号:US-2009099200-A1
优先权日:2005-06-09
标题 :Azacyclohexane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：LI CHUN SING; RAMTOHUL YEEMAN K; HUANG ZHENG; LACHANCE NICOLAS
权利人:LI CHUN SING; RAMTOHUL YEEMAN K; HUANG ZHENG; LACHANCE NICOLAS
摘要:Azacyclohexane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.

专利号:US-2010004287-A1
优先权日:2006-05-22
标题 :Cyclic Derivatives as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase
发明人：LEBLANC YVES; GAGNON MARC
权利人:MERCK FROSST CANADA LTD
摘要:Cyclic amine derivatives of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.

专利号:US-2010197692-A1
优先权日:2007-07-20
标 题 :Bicyclic heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：RAMTOHUL YEEMAN K; LI CHUN SING; LECLERC JEAN-PHILIPPE
权利人:MERCK FROSST CANADA LTD
摘要:Bicyclic heteroaromatic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis.

专利号:US-2013072495-A1
优先权日:2010-05-14
标 题 :Fused bicyclic kinase inhibitors
发明人：LI AN-HU; MULVIHILL MARK J; STEINIG ARNO G
权利人:LI AN-HU; MULVIHILL MARK J; STEINIG ARNO G; OSI PHARMACEUTICALS LLC
摘要:Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as but not limited to tumors driven at least in part by at least one of RON, MET, IR, IGF-1R, or ALK. This Abstract is not limiting of the invention.

专利号:US-8785632-B2
优先权日:2004-08-26
标 题:Enantiomerically pure aminoheteroaryl compounds as protein kinase inhibitors
发明人：CUI JINGRONG JEAN; FUNK LEE ANDREW; JIA LEI; KUNG PEI-PEI; MENG JERRY JIALUN; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; SHEN HONG; TRAN-DUBE MICHELLE
权利人:CUI JINGRONG JEAN; FUNK LEE ANDREW; JIA LEI; KUNG PEI-PEI; MENG JERRY JIALUN; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; SHEN HONG; TRAN-DUBE MICHELLE; AGOURON PHARMA; PFIZER
摘要:Enantiomerically pure compound of formula 1 n nare provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.