Brief introduction of 614731-04-3

614731-04-3 1-Boc-4-fluoro-4-piperidinecarboxylic Acid 21050397, apiperidines compound, is more and more widely used in various fields.

614731-04-3, 1-Boc-4-fluoro-4-piperidinecarboxylic Acid is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

614731-04-3, To a solution of 1- (tert-butoxycarbonyl) -4-fluoropiperidine-4-carboxylic acid (5.00 g, 20.20 mmol) in tetrahydrofuran (100 mL) was added a solution of borane tetrahydrofuran complex (30.3 mL, 30.30 mmol, 1.0 M solution in tetrahydrofuran) . The reaction mixture was refluxed for 16 hours, and then another 24 mL of borane tetrahydrofuran complex was added and continued to reflux for another 16 hours. After cooling to ambient temperature the reaction mixture poured onto ice-cold water (50 mL) and saturated ammonium chloride (100 mL) , and extracted with ethyl acetate (3 x 100 mL) , dried over anhydrous sodium sulfate and filtered. The filtrate was concentrated to afford the title compound (4.60 g, 98) . Which was used in the next step without further purification: MS (ES+) m/z 234.1 (M +1) .

614731-04-3 1-Boc-4-fluoro-4-piperidinecarboxylic Acid 21050397, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; GENENTECH, INC.; XENON PHARMACEUTICALS INC.; ANDREZ, Jean-Christophe; BICHLER, Paul Robert; CHEN, Chien-An; CHOWDHURY, Sultan; DECKER, Shannon Marie; DEHNHARDT, Christoph Martin; FOCKEN, Thilo; GRIMWOOD, Michael Edward; HEMEON, Ivan William; JIA, Qi; LI, Jun; LIU, Zhiguo; ORTWINE, Daniel F.; SAFINA, Brian; SUTHERLIN, Daniel; SHENG, Tao; SUN, Shaoyi; WHITE, Andrew D.; WILSON, Michael Scott; ZENOVA, Alla Yurevna; ZHU, Jiuxiang; WO2015/78374; (2015); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

Analyzing the synthesis route of 614731-04-3

614731-04-3 1-Boc-4-fluoro-4-piperidinecarboxylic Acid 21050397, apiperidines compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.614731-04-3,1-Boc-4-fluoro-4-piperidinecarboxylic Acid,as a common compound, the synthetic route is as follows.

tert-Butyl 4-carbamoyl-4-fluoropiperidine-1-carboxylate (0414) In a 250-mL round-bottom flask were combined 1-[(tert-butoxy)carbonyl]-4-fluoropiperidine-4-carboxylic acid (3 g, 12.13 mmol, 1.00 equiv), DMF (50 mL), NH4Cl (1.75 g, 32.72 mmol, 1.50 equiv), HATU (9.23 g, 24.27 mmol, 2.00 equiv), and iPr2NEt (3.13 g, 24.22 mmol, 2.00 equiv). The resulting solution was stirred overnight at 25 C. The resulting solution was extracted with 200 mL of EtOAc and the organic layers were combined, washed with 5¡Á50 mL of H2O, then applied onto a silica gel column with ethyl acetate/petroleum ether, affording 2.7 g (90%) of the product as a white solid., 614731-04-3

614731-04-3 1-Boc-4-fluoro-4-piperidinecarboxylic Acid 21050397, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Imago Biosciences, Inc.; Rienhoff, JR., Hugh Y.; McCall, John M.; Clare, Michael; Celatka, Cassandra; Tapper, Amy E.; (226 pag.)US2016/237043; (2016); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem