With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.103816-19-9,[1,4′-Bipiperidine]-1′-carbonyl chloride,as a common compound, the synthetic route is as follows.
To a stirred solution of fulvestrant (0.2 g) in chloroform (6 ml) and water (1 ml), sodium hydroxide (0.132 g) and tetra-n-butylammonium bromide (0.128 g) was added at room temperature and vigorously stirred at room temperature for 30 min. 4-Piperidinopiperidine-l -carbonyl chloride (0.097 g) was added to the reaction mixture and stirred at room temperature for 16 h. The reaction was monitored by TLC and LCMS. After completion of reaction, the reaction mixture was evaporated under vacuum to obtain crude material. The crude material was purified by preparative HPLC using mobile phase A) 5 mmol ammonium bicarbonate + 0.1% N in water and B) acetonitrile. Product fraction was lyophilized to afford (7R,8R,9S, l3S, l4S, l7S)-l7-hydroxy-l3- methyl-7-(9-((4,4,5,5,5-pentafluoropentyl)sulfmyl)nonyl)-7,8,9, 11, 12, 13, 14, 15, 16, l7-decahydro- 6//-cyclopenta|a|phenanthren-3-yl [l,4′-bipiperidine]-r-carboxylate (0.019 g, 7.20%) as a white solid. (0376) -NMR (400 MHz, DMSO): d 7.272 (d, 1H), 6.821 (d, 1H), 6.781 (s, 1H), 4.559 (s, 1H), 4.131 (s, 1H), 4.047 (s, 1H), 3.558 (m, 2H), 3.501-3.486 (m, 5H), 2.961 (s, 2H), 2.892-2.623 (m, 10H), 2.446-2.279 (m, 12H), 1.996-1.885 (m, 4H), 1.835-1.746 (m, 5H), 1.771-1.514 (m, 4H), 1.734- 1.601 (m, 8H), 1.525-1.262 (m, 24H), 0.901 (dd, 2H) and 0.684 (s, 3H).
103816-19-9, 103816-19-9 [1,4′-Bipiperidine]-1′-carbonyl chloride 9813375, apiperidines compound, is more and more widely used in various fields.
Reference£º
Patent; KASHIV BIOSCIENCES, LLC; PUROHIT, Parva Yogeshchandra; BRAHMKSHATRIYA, Pathik Subhashchandra; GOSWAMI, Vishalgiri Gunvantgiri; (107 pag.)WO2019/224790; (2019); A2;,
Piperidine – Wikipedia
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