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3-氟苯酚置于吡啶,三氯化铝体系中,用 二氯甲烷 用作溶剂,化学反应 0.67H,反应生成4-氟-2-羟基苯乙酮
参考文献:尿素-Pett化合物是一类新的hiv-1逆转录酶抑制剂.3. Pett类似物的合成和进一步的构效关系研究.
标题:尿素-Pett化合物是一类新的hiv-1逆转录酶抑制剂.3. Pett类似物的合成和进一步的构效关系研究.
摘要:本文描述了pett(苯乙基噻唑基硫脲)衍生物的尿素类似物系列中的变构hiv-1 Rt抑制剂的进一步开发.该系列包括具有乙基连接基(1-5)和外消旋体(6-16)和对映体(17-20)顺式环丙烷化合物的衍生物.在rt水平和细胞培养中均测定了野生型和突变型hiv-1的抗病毒活性.大多数化合物在纳摩尔范围内对wt具有抗hiv-1活性.对于某些化合物,在体外选择了抗性hiv-1,对于尿素-Pett化合物,抗性hiv-1产生的时间比参考化合物要长.大鼠的初步药代动力学显示,化合物18具有口服生物利用度,并且可以很好地渗透到大脑中.已经确定了hiv-1 Rt与两种对映体化合物(17和18)之间的复合物的三维结构.该结构在nni结合袋中显示出相似的结合.两种抑制剂的丙酰苯基部分都显示出与酪氨酸残基181和188的完美堆积.(+)-对映异构体18的环丙基部分显示出与亮氨酸残基100和缬氨酸残基179相互作用的最佳堆积距离.
Doi:10.1021/jm990095J

专利信息

专利号:CN-105294627-A
优先权日:2015-11-04
标题:A method for one-step synthesis of flavonoids catalyzed by 1,3-dialkylimidazolium oxometalates

专利号:CN-105294627-B
优先权日:2015-11-04
标 题:A method for one-step synthesis of flavonoids catalyzed by 1,3-dialkylimidazolium oxometalates

专利号:CN-116515782-A
优先权日:2022-01-24
标题:A mutant of amine dehydrogenase and its application in the synthesis of chiral aminoalcohol compounds

专利号:US-6090805-A
优先权日:1997-06-18
标 题 :Tocolytic oxytocin receptor antagonists
发明人：WILLIAMS PETER D; SPARKS MICHELLE A; BELL IAN; PERLOW DEBRA S; STAUFFER KENNETH; FREIDINGER ROGER M
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.

专利号:US-5968938-A
优先权日:1997-06-18
标 题 :Piperazine oxytocin receptor antagonists
发明人：WILLIAMS PETER D; SPARKS MICHELLE A; BELL IAN; GUARE JR JAMES P; FREIDINGER ROGER M
权利人:MERCK & CO INC
摘要:This invention relates to certain novel piperazine 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.

专利号:CN-114751870-B
优先权日:2022-02-28
标题 :A kind of 2-(isoxazol-5-yl)phenyl-3,4-dihydroxybenzoate and its derivatives and synthesis methods and applications