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CAS号13466-41-6 2-羟基-4-甲基吡啶 | CAS号695-34-1 2-氨基-4-甲基吡啶 | CAS号624-91-9 亚硝酸甲酯 | CAS号108-89-4 4-甲基吡啶 | CAS号26452-80-2 2,4-二氯吡啶 | CAS号75-16-1 甲基溴化镁 | CAS号1003-67-4 4-甲基吡啶-N-氧化物 | CAS号78948-09-1 acetyl hypofluorite | CAS号324028-95-7 6-氯-4-甲基吡啶-2-羧酸 | CAS号10026-13-8 五氯化磷 | CAS号3475-21-6 4-甲基-2-苯基吡啶 | CAS号4931-00-4 2-肼基-4-甲基吡啶 | CAS号209858-74-2 6-氯-4-甲基吡啶-2-甲腈 | CAS号102336-07-2 3-(2-甲氧基吡啶-4-基)丙酸 | CAS号102336-06-1 2-phenylmethylo... | CAS号157329-89-0 2-溴-6-氯-4-甲基吡啶 | CAS号583052-20-4 2-[3,5-bis(trif... | CAS号1134-35-6 4,4'-二甲基-2,2'-联吡啶 | CAS号101990-73-2 2-氯-4-(氯甲基)吡啶 | CAS号100848-70-2 2-甲氧基-4-甲基吡啶4-甲基吡啶氧化物置于三氯氧磷体系中,化学反应 3.0H,以64%的收率获得2-氯-4-甲基吡啶
参考文献:具有特殊亲二烯性的稳定的 2,3-吡啶反应中间体
标题:具有特殊亲二烯性的稳定的 2,3-吡啶反应中间体
摘要:据报道,2,3-吡啶 (2) 的 4-甲氧基,4-芳氧基和 4-噻吩氧基类似物 6-9 相对于 2 本身的亲二烯性增强.4-烷氧基-(22,23和25)和4-噻吩氧基-2-氯吡啶(24)在低温下的区域选择性锂化,然后消除氯化锂,得到4-烷氧基-和4-噻吩氧基吡啶,它们可以被捕获在与呋喃的 [4+2] 环加成反应中原位生成内氧化物 28-31,收率中等至非常好(25-58%).相比之下,在 C-4 处具有氢 (18) 或甲基 (12) 取代基的前体没有证据表明在这些条件下形成吡啶.由于 2-氯-6-异丙氧基-5-硫代吡啶的不稳定性,尝试从 2-氯-6-异丙氧基吡啶的低温锂化反应生成6-异丙氧基-2,3-吡啶 (10) 的尝试没有成功.
Doi:10.1002/ejoc.200400232
专利信息
专利号:US-12247037-B2
优先权日:2018-12-12
标题:1-(2,6-diazaspiro[3.3]heptan-6-yl)-5,6-dihydro-4h-benzo[f][1,2,4]triazolo[4,3-A][1,4]diazepine derivatives and related compounds as vasopressin antagonists for the treatment of neuro-psychological disorders
发明人:BRANDT GARY
权利人:NEUMORA THERAPEUTICS INC
摘要:The present invention relates to 1-(2,6-diazaspiro[3.3]heptan-6-yl)-5,6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine derivatives and related compounds of Formula (I): wherein A, B, G, R1, R1b, RiC, R2 and X are as defined herein. The present compounds are vasopressin receptor antagonists (in particular of the Via receptor) for the treatment of neuro-psychological disorders, such as e.g. autism, anxiety, stress-related disorders, depression, schizophrenia or bipolar disorder. The present description discloses the synthesis of exemplary compounds, as well as pharmacological data thereof (e.g. pages 71 to 246; examples 1 to 49; tables 1 to 5). An exemplary compound is e.g. 8-chloro-1-(2-(5-fluoropyridin-2-yl)-2,6-diazaspiro[3.3]heptan-6-yl)-5-methyl-5,6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine (example 1, compound no. 1).
专利号:US-8853410-B2
优先权日:2009-04-30
标 题:Process for preparing substituted isoxazoline compounds and their precursors
发明人:RACK MICHAEL; KOERBER KARSTEN; KAISER FLORIAN
权利人:RACK MICHAEL; KOERBER KARSTEN; KAISER FLORIAN; BASF SE
摘要:The present invention relates to a new method of preparing halogenated styrene compounds of formula (VIII) n nwhich are precursors in the process of synthesis of substituted isoxazoline compounds of formula (I)n n nwherein R 1 to R 5 , R 8 and R 9 are described as in the description.n n The present invention relates further to the synthesis of compounds of formula (I) starting from acetophenones. The desired styrenes of formula are prepared from the appropriate substituted acetophenone. Asides bromo anilines react with formoxime. Obtained oximes undergo a cycloaddition with the styrenes and give isoxazolines. Compounds of formula (I) can then be prepared in a palladium catalyzed carbonylative amination reaction of the isoxazolines.
专利号:US-6111112-A
优先权日:1999-01-22
标题 :Synthesis of 3-amino-2-chloro-4-methylpyridine from malononitrile and acetone
发明人:GROZINGER KARL
权利人:BOEHRINGER INGELHEIM PHARMA
摘要:A method for making 3-amino-2-chloro-4-methylpyridine from malononitrile, as depicted in the following reaction scheme. ##STR1##
专利号:US-8338451-B2
优先权日:2008-03-21
标 题 :Polysubstituted derivatives of 2-heteroaryl-6-phenylimidazo[1,2-a]pyridines, and preparation and therapeutic use thereof
发明人:DE PERETTI DANIELLE; EVANNO YANNICK; LARDENOIS PATRICK; MACHNIK DAVID; RAKOTOARISOA NATHALIE; ALMARIO GARCIA ANTONIO
权利人:DE PERETTI DANIELLE; EVANNO YANNICK; LARDENOIS PATRICK; MACHNIK DAVID; RAKOTOARISOA NATHALIE; ALMARIO GARCIA ANTONIO; SANOFI SA
摘要:Compounds of formula (I): n nwherein R, R 1 , R 2 , R 3 , R 4 and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.
专利号:CN-109096181-B
优先权日:2018-09-29
标题:A method for ultrasonic-assisted green synthesis of 2-sulfonylpyridine derivatives
专利号:WO-0043365-A1
优先权日:1999-01-22
标 题:Synthesis of 3-amino-2-chloro-4-methylpyridine from malononitrile and acetone