邻苯二胺置于氢氧化钾,Ppa体系中,用530 Mg (27%)的收率获得2-(4-哌啶)-1H-苯并咪唑 参考文献:Method For Treating Allergies Using Substituted Pyrazoles 标题:Method For Treating Allergies Using Substituted Pyrazoles 摘要:使用取代吡唑烷治疗过敏症状的方法,包括特应性过敏症状.
专利号:US-11370742-B2 优先权日:2018-07-24 标 题 :Process and intermediates for the preparation of bilastine 发明人:HERNÃ?NDEZ HERRERO GONZALO; GARCÃ?A DOMÃ?NGUEZ NEFTALÃ?; MORÃ?N POLADURA PABLO; GONZÃ?LEZ GARCÃ?A TANIA; GANZA GONZÃ?LEZ Ã?LVARO; TATO CERDEIRAS PALOMA 权利人:FAES FARMA SA 摘要:The invention relates to a process for preparing a compound of (III) n n n n n n n n n n n n whereinn X is a leaving group; and R 1 is C 1 -C 6 alkyl;n nwhich comprises oxidative rearrangement of a compound of formula (II) or a solvate thereofn n n n n n n n n n n n n n n n Compounds of formula (III) are key intermediates in the synthesis of Bilastine.
专利号:US-10106522-B2 优先权日:2014-12-29 标题:Benzimidazole derivatives as antihistamine agents 发明人:RODES SOLANES ROSA; OLIVERA TIZNE ROBERTO; HERNÃ?NDEZ HERRERO GONZALO; RUBIO ROYO VÃ?CTOR; LEDO GÓMEZ Francisco 权利人:FAES FARMA SA 摘要:The invention relates to compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, a method of synthesis of said compounds, pharmaceutical compositions comprising them and their use in the treatment and/or prevention of conditions mediated by H 1 histamine receptor, such as allergic disorders or diseases.
专利号:US-2008139558-A1 优先权日:2006-02-24 标题 :Quinolones useful as inducible nitric oxide synthase inhibitors 发明人:SMITH NICHOLAS D; ROPPE JEFFREY R; BONNEFOUS CELINE; PAYNE JOSEPH E; ZHUANG HUI; CHEN XIAOHONG; LINDSTROM ANDREW K; DURON SERGIO G; HASSIG CHRISTIAN A; NOBLE STEWART A 权利人:KALYPSYS INC 摘要:The present invention relates to novel quinolones of Formula I that inhibit inducible NOS synthase together with methods of synthesizing and using the compounds including methods for inhibiting or modulating nitric oxide synthesis and/or lowering nitric oxide levels in a patient by administering the compounds for the treatment of disease.
专利号:CN-117924240-A 优先权日:2023-12-26 标 题:A synthesis process of tert-butyl 4-(1H-benzo[D]imidazol-2-yl)piperidine-1-carboxylate
参考标题:Design And Synthesis Of Poly(Adp-Ribose) Polymerase Inhibitors: Impact Of Adenosine Pocket-Binding Motif Appendage To The 3-Oxo-2,3-Dihydrobenzofuran-7-Carboxamide On Potency And Selectivity 作者:Uday Kiran Velagapudi,Marie-France Langelier,Cristina Delgado-Martin,Morgan E. Diolaiti,Sietske Bakker,Alan Ashworth,Bhargav A. Patel,Xuwei Shao,John M. Pascal,Tanaji T. Talele |发布日期:2019.6.13 摘要:Poly(Adenosine 5'-Diphosphate-Ribose) Polymerase (Parp) Inhibitors Are A Class Of Anticancer Drugs That Block The Catalytic Activity Of Parp Proteins. Optimization Of Our Lead Compound 1 (( Z)-2-Benzylidene-3-Oxo-2,3-Dihydrobenzofuran-7-Carboxamide; Parp-1 Ic50 = 434 Nm) Led To A Tetrazolyl Analogue (51, Ic50 = 35 Nm) With Improved Inhibition. Isosteric Replacement Of The Tetrazole Ring With A Carboxyl
合成参考文献
摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).