With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.134676-67-8,N-Boc-2-thiomorpholinecarboxylic Acid,as a common compound, the synthetic route is as follows.
T3P (3.61 mL, 6.07 mmol) was added to a solution of 4-amino-2-chlorobenzonitrile (370 mg, 2.43 mmol), 4-(tert-butoxycarbonyl)thiomorpholine-2-carboxylic acid (500 mg, 2.02 mmol), DIEA (1.76 mL, 10.11 mmol) and DMAP (272 mg, 2.22 mmol) in ethyl acetate (10 mL) at room temperature, and the mixture was heated at 60C overnight. The reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (solvent gradient; 5?60% ethyl acetate/hexane) to give tert-butyl 2-((3-chloro-4-cyanophenyl)carbamoyl)thiomorpholine-4-carboxylate (765 mg, 2.003 mmol, 99%) as an orange oil. 1H NMR (300 MHz, CDCl3):delta 1.38-1.55(9H,m), 2.46-2.64(1H,m), 2.74-2.87(1H,m), 3.34-3.52(2H,m), 3.65(1H,dd,J=14.2,2.8 Hz), 4.03-4.17(1H,m), 4.60(1H,dd,J=14.2,4.0 Hz), 7.60(2H,d,J=3.8 Hz), 7.94(1H,s), 9.14(1H,brs)., 134676-67-8
The synthetic route of 134676-67-8 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; Takeda Pharmaceutical Company Limited; YAMAMOTO, Satoshi; SHIRAI, Junya; ODA, Tsuneo; IMADA, Takashi; KONO, Mitsunori; SATO, Ayumu; TOMATA, Yoshihide; OCHIDA, Atsuko; ISHII, Naoki; SASAKI, Yusuke; FUKASE, Yoshiyuki; YUKAWA, Tomoya; FUKUMOTO, Shoji; (200 pag.)EP3192791; (2017); A1;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem