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1. 发明申请

WO2006108689A3 PROCESS FOR PREPARING BICYCLIC COMPOUNDS 审中-公开
标题翻译：制备双相化合物的方法
公开(公告)号：WO2006108689A3
公开(公告)日：2007-02-01
申请号：PCT/EP2006003480
申请日：2006-04-06
申请人： SB PHARMCO INC , NEUROCRINE BIOSCIENCES INC , ANDREOTTI DANIELE , BACCHI SERGIO , DELPOGETTO MONICA , GUELFI SIMONE , PERBONI ALCIDE , RIBECAI ARIANNA , SPADA SIMONE , STABILE PAOLO , TAMPIERI MARSIA
发明人： ANDREOTTI DANIELE , BACCHI SERGIO , DELPOGETTO MONICA , GUELFI SIMONE , PERBONI ALCIDE , RIBECAI ARIANNA , SPADA SIMONE , STABILE PAOLO , TAMPIERI MARSIA
IPC分类号： C07D471/04 , A61K31/437 , A61P1/00 , A61P25/00 , C07D207/22
CPC分类号： C07D471/04 , C07D207/22
摘要： The present invention relates to a novel process for preparing compounds of formula (IA), which are potent and specific antagonists of corticotropin-releasing factor (CRF) receptors, from intermediate compounds of formula (I), by a coupling reaction catalysed by copper, formulae (I) (Ia) wherein X is halogen; and the other substituents are as defined in the description.
摘要翻译：本发明涉及由式（I）的中间体化合物，通过铜催化的偶联反应制备作为促肾上腺皮质激素释放因子（CRF）受体的有效和特异性拮抗剂的式（IA）化合物的新方法，式（I）（Ia）其中X是卤素; 并且其它取代基如说明书中所定义。

2. 发明申请

WO2006108693A8 PROCESS FOR PREPARING BICYCLIC COMPOUNDS 审中-公开
标题翻译：制备双相化合物的方法
公开(公告)号：WO2006108693A8
公开(公告)日：2007-10-04
申请号：PCT/EP2006003531
申请日：2006-04-06
申请人： SB PHARMCO INC , NEUROCRINE BIOSCIENCES INC , BACCHI SERGIO , DELPOGETTO MONICA , GUELFI SIMONE , PERBONI ALCIDE , RIBECAI ARIANNA , STABILE PAOLO , TAMPIERI MARSIA
发明人： BACCHI SERGIO , DELPOGETTO MONICA , GUELFI SIMONE , PERBONI ALCIDE , RIBECAI ARIANNA , STABILE PAOLO , TAMPIERI MARSIA
IPC分类号： C07D471/04 , C07D207/22
CPC分类号： C07D471/04 , C07D207/22
摘要： The present invention relates to a process for preparing compounds of formula (IA), which are potent and specific antagonists of corticotropin-releasing factor (CRF) receptors, from intermediate compounds of formula (I), by a coupling reaction catalysed by copper wherein the substituents are as defined in the claims .
摘要翻译：本发明涉及一种制备式（IA）化合物的方法，该化合物是由式（I）的中间体化合物通过铜催化的偶联反应而成为促肾上腺皮质激素释放因子（CRF）受体的有效和特异性拮抗剂，其中取代基如权利要求中所定义。

3. 发明申请

WO2006108693A2 PROCESS FOR PREPARING BICYCLIC COMPOUNDS 审中-公开
标题翻译：制备双相化合物的方法
公开(公告)号：WO2006108693A2
公开(公告)日：2006-10-19
申请号：PCT/EP2006003531
申请日：2006-04-06
申请人： SB PHARMCO INC , NEUROCRINE BIOSCIENCES INC , BACCHI SERGIO , DELPOGETTO MONICA , GUELFI SIMONE , PERBONI ALCIDE , RIBECAI ARIANNA , STABILE PAOLO , TAMPIERI MARSIA
发明人： BACCHI SERGIO , DELPOGETTO MONICA , GUELFI SIMONE , PERBONI ALCIDE , RIBECAI ARIANNA , STABILE PAOLO , TAMPIERI MARSIA
IPC分类号： C07D471/04 , C07D207/22
CPC分类号： C07D471/04 , C07D207/22
摘要： The present invention relates to a process for preparing compounds of formula (IA), which are potent and specific antagonists of corticotropin-releasing factor (CRF) receptors, from intermediate compounds of formula (I), by a coupling reaction catalysed by copper wherein the substituents are as defined in the claims.
摘要翻译：本发明涉及一种制备式（IA）化合物的方法，该化合物是由式（I）的中间体化合物通过铜催化的偶联反应而成为促肾上腺皮质激素释放因子（CRF）受体的有效和特异性拮抗剂，其中取代基如权利要求中所定义。

4. 发明申请

WO2008155334A2 IMPROVED PROCESS OF AMIDE FORMATION 审中-公开
标题翻译：改进的酰胺形成过程
公开(公告)号：WO2008155334A2
公开(公告)日：2008-12-24
申请号：PCT/EP2008057642
申请日：2008-06-18
申请人： GLAXO GROUP LTD , PERBONI ALCIDE , GIUBELLINA NICOLA
发明人： PERBONI ALCIDE , GIUBELLINA NICOLA
CPC分类号： C07D207/06
摘要： A process for the formation of 2-(methyloxy)-N-[2-methyl-1 -phenyl-2-(1 - pyrrolidinyl)propyl]-4,6-bis(trifluoromethyl)benzamide is disclosed, comprising treatment of 2,4-ditrifluoromethyl-6-methoxy-benzoic acid with an arylsulphonyl halide,C1-6alkylsulphonyl halide or di-C1-6alkylphosphoryl chloride, in the presence of a base and an aprotic solvent; followed by reaction with [2-methyl-1 -phenyl-2-(1 - pyrrolidinyl)propyl]amine or a salt thereof. Also disclosed is a process for the formation of [2-methyl-1-phenyl-2-(1- pyrrolidinyl)propyl]amine comprising: i) treatment of an a-haloketone with an alcohol in the presence of a base followed by reaction with pyrrolidine; ii) treatment of the product of stage i) with Ar-CH(R5)NH2 wherein R5 is C1-4alkyl and Ar is optionally substituted phenyl, followed by reduction with a sodium borohydride derivative; and iii) reduction of the product of stage ii) with hydrogen and a palladium catalyst. Also disclosed is the novel compound 2-pyrrolidinyl-2-methylpropiophenone or a salt or solvate thereof.
摘要翻译：公开了形成2-（甲氧基）-N- [2-甲基-1-苯基-2-（1-吡咯烷基）丙基] -4,6-双（三氟甲基）苯甲酰胺的方法，包括处理2， 4-二甲基甲基-6-甲氧基 - 苯甲酸与芳基磺酰卤，C 1-6烷基磺酰卤或二-C 1-6烷基磷酰氯在碱和非质子溶剂的存在下反应; 然后与[2-甲基-1-苯基-2-（1-吡咯烷基）丙基]胺或其盐反应。还公开了形成[2-甲基-1-苯基-2-（1-吡咯烷基）丙基]胺的方法，其包括：i）在碱的存在下用醇处理α-卤代酮，然后进行反应与吡咯烷; ii）用Ar-CH（R 5）NH 2处理步骤i）的产物，其中R 5是C 1-4烷基，Ar是任选取代的苯基，随后用硼氢化钠衍生物还原; 和iii）用氢气和钯催化剂还原阶段ii）的产物。还公开了新化合物2-吡咯烷基-2-甲基苯丙酮或其盐或溶剂化物。

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