Methanol → 4-Acryloyl-2-methoxy-2,3,4,5-tetrahydro-1,4-benzothiazepine
Reaction equation
[C:1]([N:5]1[CH2:11][C:10]2[CH:12]=[CH:13][CH:14]=[CH:15][C:9]=2[S:8][CH:7](Cl)[CH2:6]1)(=[O:4])[CH:2]=[CH2:3].[CH3:17][OH:18]>>[C:1]([N:5]1[CH2:11][C:10]2[CH:12]=[CH:13][CH:14]=[CH:15][C:9]=2[S:8][CH:7]([O:18][CH3:17])[CH2:6]1)(=[O:4])[CH:2]=[CH2:3]Participants
3
Procedure
The above-mentioned 4-acryloyl-2-chloro-2,3,4,5-tetrahydro-1,4-benzothiazepine (0.20 g), methanol (0.1 ml) and stannic chloride (0.31 g) were reacted in the same manner as in Experimental Example 13 to give 4-acryloyl-2-methoxy-2,3,4,5-tetrahydro-1,4-benzothiazepine (0.19 g). This compound (0.18 g) and 4-benzyl piperidine (0.19 g) were reacted in the same manner as in Experimental Example 5 to give 4-[3-[1-(4-benzyl)piperidinyl]propionyl]-2-methoxy-2,3,4,5-tetrahydro-1,4-benzothiazepine (0.25 g).
Sources & evidence
- ORD record
- ord-8d32cd8a25ac4f4d9399e98cef2f4d98
- Source dataset
- uspto-grants-1995_05
- Patent number
- US05416066
Reaction notes
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