CAS: 10128-91-3; Methyl 2-Oxo-1,2-Dihydro-3-Pyridinecarboxylate

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609-71-2 51146-06-6 203937-66-0

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CAS号67-56-1 甲醇 | CAS号609-71-2 2-羟基烟酸 | CAS号393-55-5 2-氟烟酸 | CAS号28369-76-8 2-hydroxynicoti... | CAS号78686-79-0 5-溴-2-氯烟酸甲酯 | CAS号78686-83-6 2-氯-5-碘烟酸甲酯 | CAS号116387-40-7 2-羟基-5-碘烟酸甲酯 | CAS号120034-05-1 5-溴-2-羟基烟酸甲酯 | CAS号153336-74-4 3-Pyridinecarbo... | CAS号67367-27-5 1-甲基-2-氧-1,2-二氢... | CAS号868171-67-9 1-(4-氟苯基)-2-氧代-...

📜2-羟基烟酸置于氯化亚砜,N,N-二甲基甲酰胺体系中,用 四氢呋喃 用作溶剂,化学反应 2.5H,反应生成2-氧代-1,2-二氢-3-吡啶羧酸甲酯
参考文献:具有手性6,7-反式-双取代-1,4-恶唑烷的支架的周边选择性去甲肾上腺素再摄取抑制剂的实用合成的发展.
标题:具有手性6,7-反式-双取代-1,4-恶唑烷的支架的周边选择性去甲肾上腺素再摄取抑制剂的实用合成的发展.
摘要:描述了具有手性6,7-反式-二取代-1,4-氧杂庚烷作为新型支架的外围选择性去甲肾上腺素再摄取抑制剂的实用合成.具有优异的立体化学的氨基醇是通过优异的dr和ee获得的,它是通过morita-Baylis-Hillman反应,Michael加成,马来酸盐的分离,还原和与(+)-的非对映异构体盐的形成,从市场上可买到的醛中获得的. 10-樟脑磺酸.在合成的早期阶段获得的所需单一立体异构体在完全伸缩的过程中用于七元环的形成,从而有效地提供了手性6,7-反式-二取代-1,4-氧杂庚烷.除了控制手性1,4-恶唑烷的dr和ee以及控制中间体甲磺酸酯与吡啶酮衍生物在s N 2反应中的n,O选择性,找到适合分离和纯度提高的合适中间体,从而可以实现无手性HPLC分离,无柱色谱的药物候选物的实用合成.非常好的化学和光学纯度,总收率更高.
Doi:10.1021/acs.Oprd.7B00313

专利信息

专利号:US-6258323-B1
优先权日:1998-11-16
标题:Apparatus and method used in multiple, simultaneous synthesis of general compounds
发明人：HORMANN ROBERT EUGENE; GILBERT DARYL EUGENE; SIOMA EDWARD MICHAEL
权利人:ROHM & HAAS
摘要:The apparatus and method of the present invention provides for conducting simultaneous multiple synthesis of general compounds, which often takes place under varied uneven conditions requiring heating, cooling, agitation, reagent/solvent additions to the reactor contents at each reaction vessel location, supply and maintenance of inert atmosphere and means to facilitate the reflux of the reactor contents. Thus, it becomes necessary to monitor and control the reaction conditions during the simultaneous multiple synthesis of general compounds. The apparatus allows the user to connect various independently controlling and conveying means to each reaction vessel through multiple ports provided on a stopper mounted on each reaction vessel. The apparatus of the present invention permits user to readily access the reaction vessels without interrupting the reactions occurring in the adjacent reaction vessels. The unique geometry and shape of the stopper allows positioning of multiple ports, while still providing the stopper with a compact size. As a result, a large array of reaction vessels can be accommodated in the device of the present invention without significantly increasing the overall size of the apparatus. Some of the general compounds that can be readily synthesized by the apparatus and the method of the present invention include inorganic compounds as well as organic compounds, such as oligomers, polymers, agricultural chemicals, drugs, peptides and oligonucleotides.