Formaldehyde → tert-Butyl 7-Methyl-5,6,7,8-tetrahydro-[1,2,4]triazolo[1,5-a]pyrazin-2-yl-carbamate
반응식
[N:1]1[C:2]([NH:10][C:11](=[O:17])[O:12][C:13]([CH3:16])([CH3:15])[CH3:14])=[N:3][N:4]2[CH2:9][CH2:8][NH:7][CH2:6][C:5]=12.C=O.[BH3-][C:21]#N.[Na+]>[Cl-].[Cl-].[Zn+2].C(OCC)C.CO>[CH3:21][N:7]1[CH2:8][CH2:9][N:4]2[N:3]=[C:2]([NH:10][C:11](=[O:17])[O:12][C:13]([CH3:14])([CH3:16])[CH3:15])[N:1]=[C:5]2[CH2:6]1참가 물질
6
반응물 3
생성물 1
시약·촉매·용매 2
실험 절차
Following the procedure in Example 191i, and starting with 270d (500 mg, 2.1 mmol, 1.0 eq.), paraformaldehyde (630 mg, 21.0 mmol, 10.0 eq.), ZnCl2/diethyl ether (2.1 mL, 2.1 mmol, 1.0 M), NaBH3CN (390 mg, 6.3 mmol, 3.0 eq.), and methanol (20 mL) afforded 270e as a yellow solid (500 mg, 94%). MS-ESI: [M-tBu]+ 198.0.
출처 및 근거
- ORD 기록
- ord-5fd60e60d04846c0aefd94d9c18ec8f3
- 출처 데이터셋
- uspto-grants-2014_05
- 특허 번호
- US08716274B2
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