Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 134676-67-8, name is N-Boc-2-thiomorpholinecarboxylic Acid. This compound has unique chemical properties. The synthetic route is as follows. 134676-67-8
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).
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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