CAS: 3222-49-9; 5-Methylnicotinic Acid

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29681-45-6 100910-66-5 102074-19-1

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CAS号591-22-0 3,5-二甲基吡啶 | CAS号42972-46-3 1-(5-甲基吡啶-3-基)乙酮 | CAS号612-58-8 3-甲基喹啉 | CAS号112945-08-1 3-methyl-5-pent... | CAS号7732-18-5 水 | CAS号455-70-9 5-氟吡啶-3-甲酸甲酯 | CAS号407-21-6 3-氟-5-甲基吡啶 | CAS号3430-19-1 3-氨基-5-甲基吡啶 | CAS号39891-04-8 5-氟吡啶-3-甲醛 | CAS号402-66-4 5-氟烟酸 | CAS号20970-77-8 2-Pyridinecarbo... | CAS号70-57-5 5-甲基烟酰氨 | CAS号884494-95-5 5-甲基-3-羧酸氯吡啶 | CAS号20826-02-2 5-甲基烟酸乙酯 | CAS号102074-19-1 (5-甲基吡啶-3-基)甲醇

3,5-二甲基吡啶置于potassium Permanganate体系中,化学反应 20.0H,以41%的收率获得产物5-甲基烟酸
参考文献:[(3-吡啶基烷基)哌啶]苯并环庚吡啶衍生物作为paf和组胺的双重拮抗剂.
标题:[(3-吡啶基烷基)哌啶]苯并环庚吡啶衍生物作为paf和组胺的双重拮抗剂.
摘要:制备了一系列的[(3-吡啶基烷基)哌啶基]-和(烟酰基哌啶基)苯并环庚吡啶衍生物ia,B,并评价了paf拮抗剂和h1抗组胺活性.通过体外paf诱导的血小板聚集测定(ppa)和体内paf诱导的大鼠低血压测试(ph)和小鼠的死亡率测试(pm),研究了paf拮抗剂的活性.为了评估h1抗组胺药的活性,在血压正常的大鼠中使用了体外组胺引起的豚鼠回肠试验(hc)收缩和体内组胺引起的低血压试验(hh).使用活性过敏性休克试验在小鼠中评估了化合物的潜在抗过敏活性.这些化合物在结构上与氯雷他定(1)有关,是通过用取代的3-吡啶基甲基和烟酰基部分取代1的乙氧羰基而反应生成的.抗paf和h1抗组胺活性均显示出对吡啶环中取代基的确切性质和位置的高度依赖性.结合有(5-甲基-3-吡啶基)甲基的最佳结构19(ur-12592)表现出独特的双重活性,可抑制两种paf诱导的作用(ppa,Ic50 = 3.7 Microm; Ph,Id50
DOI:10.1021/jm00043A009

专利信息

专利号:US-6803468-B2
优先权日:2000-08-29
标 题 :Process for the synthesis of n-(5-methylnicontinoyl)-4 hydroxypiperidine, a key intermediate of rupatadine
发明人：KUMAR YATENDRA; PRASAD MOHAN; SINGH SHAILENDRA KUMAR
权利人:RANBAXY LAB LTD
摘要:The present invention relates to an improved and industrially advantageous process for the preparation of N-(5-methylnicotinoyl)-4-hydroxypiperidine of Formula I, as shown in the accompanied drawings. This compound is a key intermediate for the synthesis of rupatadine, a potent dual antagonist of histamine and platelet-activating factor (PAF).

专利号:US-2006116519-A1
优先权日:2004-11-17
标 题:Synthesis of 5-bromo-4-methyl-pyridin-3-ylmethyl)-ethyl-carbamic acid tert-butyl ester
发明人：MA CHUNRONG; TIAN QINGPING
权利人:AGOURON PHARMA
摘要:The present invention relates to novel synthetic methods for the preparation of intermediates of 3{5-[3-(4,6-Difluoro-1H-benzoimidazol-2-yl)-1H-indazol-5-yl]4-methyl-pyridin-3-yl methyl}-ethyl-amine.

专利号:US-2004044216-A1
优先权日:2000-08-29
标题 :Process for the synthesis of n-(5-methylnicotinoyl)-4 hydroxypiperidine, a key intermediate of rupatadine

专利号:US-9938278-B2
优先权日:2014-12-17
标题 :FXR (NR1H4) modulating compounds
发明人：GEGE CHRISTIAN; KREMOSER CLAUS; KINZEL OLAF; BLOMGREN PETER A; CURRIE KEVIN S; KROPF JEFFREY E; SCHMITT AARON C; WATKINS WILLIAM J; XU JIANJUN
权利人:GILEAD SCIENCES INC
摘要:The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

专利号:US-2010004245-A1
优先权日:2006-10-20
标 题:Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：OBALLA RENATA M; DESCHENES DENIS; GAGNON MARC; LEBLANC YVES; POWELL DAVID; RAMTOHUL YEEMAN K
权利人:MERCK FROSST CANADA LTD
摘要:Azacycloalkane derivatives 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.

专利号:EP-3515880-B1
优先权日:2017-03-17
标题:Methods and compositions for synthesis of encoded libraries
发明人：LI JIN; MORGAN BARRY A; Wan jinqiao; DOU DENGFENG; LIU GUANSAI; CHANG YONG; CHEN QIUXIA; WANG XING; XU YANSHAN; HU DONGYAN; LIU JIAN; CHENG XUEMIN
权利人:HITGEN INC