CAS: 282526-98-1; 2-(Hexadecyloxy)-6-Methyl-4H-Benzo[d][1,3]Oxazin-4-One

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CAS号890655-08-0 新利司他原料中间体 | CAS号541-41-3 氯甲酸乙酯

Hexadecanyl P-Trifluoromethylsulfonate置于三乙胺体系中,用 二氯甲烷 用作溶剂,以90%的收率获得新利司他
参考文献:一种以2-氨基-5-甲基苯甲酸为原料高效合成cetilistat的工艺
标题:一种以2-氨基-5-甲基苯甲酸为原料高效合成cetilistat的工艺
摘要:本发明公开了一种以2‑氨基‑5‑甲基苯甲酸为原料高效合成cetilistat的工艺,是以2‑氨基‑5‑甲基苯甲酸为原料,与三光气在有机碱催化的作用下发生酯交换反应生成中间体c--6‑甲基‑2,4‑二氢‑1H‑‑3,1‑苯并恶嗪‑2,4‑二酮;再采用特定结构的磺酰氯(D),在碱催化的条件下与正十六醇反应生成中间体f;最后,中间体c和中间体f在有机碱存在下发生氧原子上的烷基化反应生成目标产物cetilistat.本发明合成cetilistat反应步骤少,工艺路线短,副反应少,最终产品收率高,纯度>99%.

专利信息

专利号:US-10005720-B2
优先权日:2013-04-05
标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
发明人：SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

专利号:US-2018370905-A1
优先权日:2013-04-05
标题:Compounds Useful for the Treatment of Metabolic Disorders and Synthesis of the Same

专利号:US-2011301143-A1
优先权日:2009-02-23
标题 :Heterocyclic derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：ISABEL ELISE; LACHANCE NICOLAS; LECLERC JEAN-PHILIPPE; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; RAMTOHUL YEEMAN K; ROY PATRICK; TRANMER GEOFFREY K; ASPIOTIS RENEE; LI LIANHAI; MARTINS EVELYN
权利人:ISABEL ELISE; LACHANCE NICOLAS; LECLERC JEAN-PHILIPPE; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; RAMTOHUL YEEMAN K; ROY PATRICK; TRANMER GEOFFREY K; ASPIOTIS RENEE; LI LIANHAI; MARTINS EVELYN
摘要:Heterocyclic compounds of structural formula (I), or a pharmaceutically acceptable salt thereof, wherein W is a R1— substituted heteroaryl, R1 is an heteroaryl ring substituted with an ester or carboxylic acid containing radical, X-T is N—CR5R6, Câ• CR5 or CR13—CR5R6, Y is a bond or —C(O)—, a and b represent an integer selected from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The heterocyclic compounds 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, cancer, liver steatosis, and non-alcoholic steatohepatitis.

专利号:US-2011183958-A1
优先权日:2008-10-17
标 题 :Azetidine derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：POWELL DAVID; TRANMER GEOFFREY K
权利人:MERCK FROSST CANADA LTD
摘要:Azetidine derivatives 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; cancer; liver steatosis; and non-alcoholic steatohepatitis.

专利号:US-2012010186-A1
优先权日:2009-03-23
标题:Heterocyclic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：LACHANCE NICOLAS; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; TRANMER GEOFFREY K; MARTINS EVELYN; GAREAU YVES
权利人:LACHANCE NICOLAS; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; TRANMER GEOFFREY K; MARTINS EVELYN; GAREAU YVES; MERCK FROSST CANADA LTD
摘要:Heterocyclic 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; cancer, liver steatosis; and non-alcoholic steatohepatitis.

专利号:US-2011152295-A1
优先权日:2008-09-08
标 题:Heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：LECLERC JEAN-PHILIPPE; LI CHUN SING; RAMTOHUL YEEMAN K
权利人:LECLERC JEAN-PHILIPPE; LI CHUN SING; RAMTOHUL YEEMAN K
摘要:Heteroaromatic compounds 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.