(4S)-4-Cyclohexyl-L-proline

Compound V (1.2 g), 5percent Rhodium on charcoal (0.24 g), concentrated hydrochloric acid (1.2 ml) and methanol (12 ml) were added to the reaction flask. The mixture was stirred and hydrogenated at 2.0 MPa with hydrogen and heated to 30 .After the reaction was performed for 2h, the reaction mixture was filtered under reduced pressure. The filtrate was concentrated under reduced pressure to give a white solid (1.11 g). Yield: 90.0percent.Compound III (0.71 kg) was dissolved in dichloromethane (13 L) in a reaction flask and pyridine (6.23 g) was added with stirring. And triethylamine (204.4 g). The reaction solution was cooled to -10 to -15 C under ice-salt bath, pivaloyl chloride (243.6 g) was added dropwise and the mixture was stirred at 2hWithin the drop is completed. After the addition was completed, the system temperature was maintained at -10 C ~ -15 C for 2h, and then compound IV (362.2 g), heated with stirring to 20 ~ 25 , TLC monitoring, stirring the reaction 2h, the reaction was added purified water (15.5 L), pH = 1.0 ~ 2.0 with hydrochloric acid (6N, 500 mL), stirred for 10 min and allowed to stand for 10 min. Phase, repeated washing twice. The organic phase was concentrated under reduced pressure in vacuo to give the oil fosinopril (temperature controlled at 25-30 C), heavy594g, yield 57.1%.Compound V (1.2 g), 5% Rhodium on charcoal (0.24 g), concentrated hydrochloric acid (1.2 ml) and methanol (12 ml) were added to the reaction flask. The mixture was stirred and hydrogenated at 2.0 MPa with hydrogen and heated to 30 .After the reaction was performed for 2h, the reaction mixture was filtered under reduced pressure. The filtrate was concentrated under reduced pressure to give a white solid (1.11 g). Yield: 90.0%.

Molecular Weight:197.27
XLogP3:0.3
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:3
Rotatable Bond Count:2
Exact Mass:197.141578849
Monoisotopic Mass:197.141578849
Topological Polar Surface Area:49.3
Heavy Atom Count:14
Complexity:211
Defined Atom Stereocenter Count:2
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes