CAS: 120277-68-1; 3-(Chloromethyl)-2-Methylpyridine

该化合物是属于类丙烯衍生物的有机化合物,具有由六人组成的芳香热循环环,含有一个氮原子;该化合物的特征是,在三处有一个氯甲基组(-CH2Cl),在2处放置在环上有一个甲基组(-CH3),这种替代模式影响其再活动性和有机合成中的潜在应用;已知的衍生物具有多种生物活动,可作为合成药物,农用化学品和其他精细化学品的中间体;该氯甲基组可以参与核分裂替代反应,使这种化合物在进一步的化学转化中有用;此外,对丙烯化合物一般表现出中度至高极度,可能影响其在各种溶剂中的溶解性.应当参考安全数据处理,因为卤化化合物可能对健康造成危害.

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相似化合物

4370-22-3 27221-49-4 58539-77-8

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CAS号56826-61-0 3-羟甲基-2-甲基吡啶 | CAS号1721-26-2 2-甲基烟酸乙酯 | CAS号60032-57-7 2-甲基吡啶-3-甲醛 | CAS号65719-09-7 2-甲基烟酸甲酯 | CAS号101166-73-8 2-甲基-3-吡啶乙腈 | CAS号162046-68-6 3-(chloromethyl...

合成工艺路线路线简述

    📜3-羟甲基-2-甲基吡啶置于氯化亚砜体系中,用 二氯甲烷 用作溶剂,化学反应 4.0H,以74%的收率获得3-(氯甲基)-2-甲基吡啶
    参考文献:口服活性催产素拮抗剂的开发:1-(1-[1-[4-[1-(2-甲基-1-氧吡啶基-3-基甲基)哌啶-4-基氧基]-2-甲氧基苯甲酰基]哌啶-4-基)的研究-1,4-二氢苯并[d] [1,3]恶嗪-2-酮(l-372,662)和相关的吡啶.
    标题:口服活性催产素拮抗剂的开发:1-(1-[1-[4-[1-(2-甲基-1-氧吡啶基-3-基甲基)哌啶-4-基氧基]-2-甲氧基苯甲酰基]哌啶-4-基)的研究-1,4-二氢苯并[d] [1,3]恶嗪-2-酮(l-372,662)和相关的吡啶.
    摘要:先前报道的催产素拮抗剂l-371,257(2)在其乙酰基哌啶末端进行了修饰,以结合各种吡啶n-氧化物基团.这种修饰导致鉴定出具有改善的药代动力学和优异的口服生物利用度的化合物.吡啶n-氧化物系列的实例为l-372,662(30),在体外和体内(大鼠体内静脉ad50 = 0.71 Mg / Kg)(ki = 4.1 Nm,克隆的人催产素受体)均具有非常好的效价.口服生物利用度(在大鼠中为90%,在狗中为96%),非常好的水溶解度(在ph 5.2下> 8.5 Mg / Ml)应有利于静脉内给药的制剂以及对人精氨酸加压素受体的优异选择性.在这类催产素拮抗剂中,在中央苯甲酰基环上引入5-氟取代基可增强体外和体内效能,但不利于这些化合物的药代动力学.尽管在化合物30的吡啶环周围的亲脂取代在体外具有更高的亲和力,但是这种取代基是代谢缺陷,并导致体内的不足.研究了两种防止这种新陈代谢的方法,即增加循环限制和
    Doi:10.1021/jm9800797

    海关参考信息

    专利信息


    专利号:WO-9725992-A1
    优先权日:1996-01-16
    标 题 :Tocolytic oxytocin receptor antagonists
    发明人:SPARKS MICHELLE A; FRIEDINGER ROGER M; PERLOW DEBRA S; WILLIAMS PETER D
    权利人:MERCK & CO INC; SPARKS MICHELLE A; FRIEDINGER ROGER M; PERLOW DEBRA S; WILLIAMS PETER D
    摘要:This invention relates to certain novel benzoxazinone compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery.

    专利号:US-5726172-A
    优先权日:1996-01-16
    标题 :Tocolytic oxytocin receptor antagonists
    发明人:SPARKS MICHELLE A; FREIDINGER ROGER M; PERLOW DEBRA S; WILLIAMS PETER D
    权利人:MERCK & CO INC
    摘要:This invention relates to certain novel benzoxazinone compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery. A typical compound is as follows:

    专利号:US-5756497-A
    优先权日:1996-03-01
    标题 :Tocolytic oxytocin receptor antagonists
    发明人:BELL IAN M; FREIDINGER ROGER M; WILLIAMS PETER D
    权利人:MERCK & CO INC
    摘要:This invention relates to certain novel benzoxazinone compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor in mammals, especially humans. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery.

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