Downstream synthetic route of 782501-25-1

As the paragraph descriping shows that 782501-25-1 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.782501-25-1,1-Boc-4-Chlorosulfonylpiperidine,as a common compound, the synthetic route is as follows.,782501-25-1

Example 128 and 129: tert-Butyl 4-(N-(5-(2-methoxyphenyl)-1,3,4-thiadiazol-2- yl)sulfamoyl)piperidine-1-carboxylate, 128 and N-(5-(2-methoxyphenyl)-1,3,4- thiadiazol-2-yl)piperidine-4-sulfonamide hydrochloride, 129 a) tert- butyl 4-(N-(5-(2-methoxyphenyl)-1,3,4-thiadiazol-2-yl)sulfamoyl)piperidine-1- carboxylate 128 Lithium bis(trimethylsilyl)amide solution 1.0 M in THF (0.386 mL, 0.386 mmol) was added to a solution of 5-(2-methoxyphenyl)-1,3,4-thiadiazol-2-amine 1109 (0.040 g, 0.193 mmol) in tetrahydrofuran (1.93 mL) at -10 C and the reaction was stirred for 10 min. A solution of tert-butyl 4-chlorosulfonylpiperidine-1-carboxylate (0.066 g, 0.232 mmol) in THF (0.5 mL) was added dropwise, the resulting mixture was warmed to room temperature and stirred overnight. The reaction was quenched with water (5 mL), acidified with 1 M HCI and extracted with EtOAc (3 x 10 mL). The combined organics were washed with brine, dried (MgS04) and concentrated. Purification by column chromatography (4 g silica cartridge, 50- 90% ethyl acetate in petroleum benzine 40-60 C) gave the title compound (0.013 g, 15% yield) as a pale yellow oil. LCMS-C: rt 6.14 min, m/z 453.2 [M-H]-, NMR (400 MHz, CDCIs) d 8.07 (dd, J = 7.9, 1.7 Hz, 1H), 7.47 (ddd, J = 8.4, 7.4, 1.7 Hz, 1H), 7.07 (td, J =7.6, 1.0 Hz, 1H), 7.02 (d, J = 8.4 Hz, 1H), 4.34-4.18 (m, 2H), 3.98 (s, 3H), 3.16 (tt, J = 1 1.9, 3.6 Hz, 1H), 2.80-2.69 (m, 2H), 2.17 (dd, J = 13.6, 3.6 Hz, 2H), 1.77 (qd, J = 12.5, 4.5 Hz, 2H), 1.46 (s, 9H).

As the paragraph descriping shows that 782501-25-1 is playing an increasingly important role.

Reference£º
Patent; CTXT PTY LIMITED; STUPPLE, Paul, Anthony; LAGIAKOS, Helen, Rachel; FOITZIK, Richard, Charles; CAMERINO, Michelle, Ang; NIKOLAKOPOULOS, George; BOZIKIS, Ylva, Elisabet, Bergman; KERSTEN, Wilhelmus, Johannes, Antonius; WALKER, Scott, Raymond; HUBERT, Jonathan, Grant; (0 pag.)WO2020/2587; (2020); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

Simple exploration of 782501-25-1

782501-25-1 1-Boc-4-Chlorosulfonylpiperidine 45789737, 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.782501-25-1,1-Boc-4-Chlorosulfonylpiperidine,as a common compound, the synthetic route is as follows.

782501-25-1, A solution of tert-butyl 4-(chlorosulfonyl)piperidine-1-carboxylate (3.000 g, 10.572 mmol) in dichloromethane (50 mL) was mixed at the room temperature with 3-chloroaniline (1.618 g, 12.686 mmol) and triethylamine (2.210 mL, 15.858 mmol), and stirred at the same temperature for 18 hr. Then, water was added to the reaction mixture, followed by extraction with dichloromethane. The organic layer was washed with aqueous saturated sodium chloride solution, dried with anhydrous Mg504, filtered, and concentrated in vacuo. The residue was chromatographed (5i02, 40 g cartridge; ethyl acetate / hexane = 20 % to 50 %) to give the concentrate, and then the concentrate was dissolved in ethyl acetate (10 mL) and hexane (100 mL) and stirred. The resulting precipitates were collected by filtration, washed by hexane, and dried to give tert-butyl 4-(N-(3-chlorophenyl)sulfamoyl)piperidine- 1-carboxylate as white solid(0.860 g, 21.7 %).

782501-25-1 1-Boc-4-Chlorosulfonylpiperidine 45789737, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; LEE, Jaekwang; HAN, Younghue; KIM, Yuntae; CHOI, Daekyu; MIN, Jaeki; BAE, Miseon; YANG, Hyunmo; KIM, Dohoon; (644 pag.)WO2017/18803; (2017); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem