CAS: 104641-59-0; (S)-(+)-1-Methyl-3-Pyrrolidinol

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104641-60-3 13220-33-2 100858-32-0

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CAS号1104643-24-4 (S)-3-tert-buto... | CAS号50-00-0 甲醛 | CAS号122536-94-1 (S)-3-羟基吡咯烷盐酸盐 | CAS号104612-35-3 (S)-(-)-2-羟基-N-...

📜(S)-(-)-2-羟基-N-甲基琥珀酰亚胺置于红铝体系中,用 四氢呋喃,甲苯 用作溶剂,化学反应 1.0H,以64%的收率获得(S)-(+)-1-甲基-3-羟基吡咯烷
参考文献:罗卡汀和其类似物的旋光异构体:其对映异构体的合成和h1抗组胺活性及其与经典抗组胺剂的结构关系.
标题:罗卡汀和其类似物的旋光异构体:其对映异构体的合成和h1抗组胺活性及其与经典抗组胺剂的结构关系.
摘要:2-[2-(二甲基氨基)乙基]-3,4-二氢-4-甲基吡啶并[3,2-F]-1,4-氧杂氮平-5(2H)-硫酮(罗卡汀)的对映体及其两个制备了更强效的类似物,其对映体纯度大于99.9%.通过这些化合物在豚鼠中阻断组胺诱导的致死性和抑制[3H]美吡拉明与豚鼠皮层结合的能力来评估其抗组胺活性.在该系列中,在2位具有r构型的化合物的效力至少是s异构体的300倍.构象分析和分子建模表明,罗卡汀可以采用一种构象,其中吡啶环,醚氧和质子化胺官能团的位置与某些更经典的抗组胺药可能结合的构象异构体的相应元素相似.这个构象,
Doi:10.1021/jm00108A012

专利信息

专利号:US-10975101-B2
优先权日:2016-05-31
标题:Ultra-potent vinca alkaloids: added molecular complexity further disrupts the tublin dimer-dimer interface
发明人：BOGER DALE
权利人:SCRIPPS RESEARCH INST
摘要:Synthetically-derived and previously inaccessible modifications of 20′-hydroxy-vinca derivative compounds such as vinblastine, vincristine or vindesine are disclosed that are a stunning 100-fold more active than the natural product (IC 50 's 50-75 pM vs 7 nM, HCT116), and are now accessible as a result of advances in the total synthesis of the natural product. Illustrative new ultra-potent vinblastines bind tubulin with much higher affinity and likely further disrupt the tubulin head-to-tail α/β dimer-dimer interaction by virtue of the strategic placement of an added conformationally well-defined, rigid and extended C20′-urea along the adjacent protein-protein interface. Added molecular complexity was used to markedly enhance target binding and functional biological activity, and represents a general approach to improving the properties of other natural products targeting a protein-protein interaction. A pharmaceutical composition containing an ultra-potent 20′-hydroxy-vinca derivative compound and a method of treating cancerous cells with such a compound are also disclosed.