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异戊酸置于二苯基磷酸,三乙胺体系中,用 甲苯 用作溶剂,化学反应 1.5H,反应生成异氰酸异丁酯
参考文献:发现在6-位带有对甲氧基脲基苯基部分的噻吩并[2,3-D]嘧啶-2,4-二酮:一种用于人类促黄体生成激素释放激素受体的高效且可口服生物利用的非肽拮抗剂.
标题:发现在6-位带有对甲氧基脲基苯基部分的噻吩并[2,3-D]嘧啶-2,4-二酮:一种用于人类促黄体生成激素释放激素受体的高效且可口服生物利用的非肽拮抗剂.
摘要:我们先前已经公开了第一种有效且口服有效的非肽类抗人黄体生成激素释放激素(lhrh)受体,即噻吩并[2,3-B]吡啶-4-酮衍生物t-98475(1).已经通过采用用其他杂环代用品替代噻吩并吡啶-4-酮核的策略对开发非肽lhrh拮抗剂进行了广泛的研究.我们在本文中描述了一系列含有联芳基部分的噻吩并[2,3-D]嘧啶-2,4-二酮衍生物的设计和合成,这些衍生物导致发现了一种高效且口服活性的非肽lhrh拮抗剂,5-(n-苄基-N-甲基氨基甲基)-1-(2,6-二氟苄基)-6-[4-(3-甲氧基脲基)苯基]-3-苯基噻吩并[2,3-D]嘧啶-2,4(1H,3H)-二酮(9K:Tak-013).化合物9K对人受体显示出高结合亲和力和有效的体外拮抗活性,其最大抑制浓度(ic(50))值分别为0.1和0.06 Nm.口服9K能够以30 Mg / Kg的剂量在cast割的雄性食蟹猕猴中几乎完全抑制
Doi:10.1021/jm020180I

专利信息

专利号:US-4366317-A
优先权日:1981-06-22
标题 :Process for synthesis of N-(hydrocarbyl)substituted-p-menthane-3-carboxamide
发明人：HAUT STEPHEN A; COMES ROGER A
权利人:PHILIP MORRIS INC
摘要:This invention provides an improved process for synthesizing carboxamides which involves reacting 3-p-menthyl halide with magnesium to form 3-p-menthylmagnesium halide Grignard reagent, and reacting the Grignard reagent with hydrocarbyl isocyanate at a temperature below about -20 DEG C. to form N-hydrocarbyl-p-menthane-3-carboxamide product. The product comprises a mixture of geometric isomers in which the 3-p-menthyl:3-p-neomenthyl weight ratio is at least 4:1 and can be as high as 9:1 under optimal conditions. This invention also provides a novel process for producing acylurea compounds such as N-(3-p-menthylcarbonyl)-N-t-butyl-N'-t-butylurea.

专利号:US-2021087191-A1
优先权日:2020-12-04
标 题 :SUBSTITUTED 3-ISOBUTYL-9,10-DIMETHOXY-1,3,4,6,7,11B-HEXAHYDRO-2H-PYRIDO[2,1-a]ISOQUINOLIN-2-OL COMPOUNDS, THEIR SYNTHESIS, AND USE THEREOF
发明人：MILLER DAVE ALAN; ELLENBERGER DANIEL J; GUNIC ESMIR; GIRARDET JEAN-LUC; SPANGENBERG ANGELA
权利人:DISPERSOL TECHNOLOGIES LLC
摘要:The invention relates to substituted 3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-ol compounds, their synthesis, pharmaceutical compositions containing them, and methods of using them in the treatment of disorders benefiting from inhibition of vesicular monoamine transporter 2 (VMAT2).

专利号:EP-3143060-B1
优先权日:2014-05-12
标题 :Catalysts for the synthesis of oxazolidinone compounds

专利号:US-2017081462-A1
优先权日:2014-05-12
标 题 :Catalysts for the synthesis of oxazolidinone compounds

专利号:US-2017088659-A1
优先权日:2014-05-12
标题 :Catalysts for the synthesis of oxazolidinone compounds

专利号:EP-3143059-B1
优先权日:2014-05-12
标 题:Catalysts for the synthesis of oxazolidinone compounds
发明人：MÃœLLER THOMAS ERNST; Gürtler Christoph; BASU SUSMIT; RANGHEARD CLAUDINE; WEBER ANNA; VOGT HENNING; LEITNER WALTER
权利人:COVESTRO DEUTSCHLAND AG