Diisopropylethylamine → HCID 178493855, 화합물

HRID 1259504

반응식

HRID 1259504 반응식
[CH3:1][O:2][C:3]1[C:12]2[N:11]=[C:10]([NH2:13])[N:9]3[CH2:14][CH2:15][N:16]=[C:8]3[C:7]=2[CH:6]=[CH:5][C:4]=1[O:17][CH2:18][CH2:19][CH2:20][N:21]1[CH2:26][CH2:25][O:24][CH2:23][CH2:22]1.[NH2:27][C:28]1[CH:33]=[C:32]([C:34](O)=[O:35])[CH:31]=[CH:30][N:29]=1.C1CN([P+](ON2N=NC3C=CC=CC2=3)(N2CCCC2)N2CCCC2)CC1.F[P-](F)(F)(F)(F)F.C(N(C(C)C)CC)(C)C>CN(C=O)C>[NH2:27][C:28]1[CH:33]=[C:32]([CH:31]=[CH:30][N:29]=1)[C:34]([NH:13][C:10]1[N:9]2[CH2:14][CH2:15][N:16]=[C:8]2[C:7]2[CH:6]=[CH:5][C:4]([O:17][CH2:18][CH2:19][CH2:20][N:21]3[CH2:22][CH2:23][O:24][CH2:25][CH2:26]3)=[C:3]([O:2][CH3:1])[C:12]=2[N:11]=1)=[O:35]

참가 물질

6

반응물 4

HCID 81531DiisopropylethylamineHCID 2783962-Aminopyridine-4-carboxylic acidHCID 2724699PyBOPHCID 178493860HCID 178493860, 화합물

생성물 1

HCID 178493855HCID 178493855, 화합물수율 37.2%

시약·촉매·용매 1

HCID 6228Dimethylformamide용매

실험 절차

7-Methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-amine (100 mg, 0.28 mol) was dissolved in DMF (3 mL), and 2-aminopyridine-4-carboxylic acid (38 mg, 0.28 mmol) was added. PYBOP (217 mg, 0.42 mmol) and diisopropylethylamine (0.15 mL, 0.83 mmol) were subsequently added, and the mixture was stirred at rt overnight. The mixture was purified by HPLC to give the title compound (50 mg, 37%). LC MS RT=1.02 min, MH+=480.3. 1H NMR (DMSO-d6) δ: 13.25 (1H, br s), 10.15 (1H, br s), 8.42 (1H, br s), 8.08 (1H, s), 8.06 (1H, d), 7.43 (1H, d), 7.75 (1H, s), 7.50 (1H, d), 7.38 (1H, dd), 4.50 (2H, dd), 4.35 (2H, br t), 4.27 (2H, dd), 4.01 (3H, s), 3.99 (2H, br s), 3.66 (2H, t), 3.50 (2H, d), 3.31 (2H, br t), 3.13 (2H, m), 2.25 (2H, m).

후처리

  1. customThe mixture was purified by HPLC

출처 및 근거

ORD 기록
ord-1b09de3ca90845aeb5718273284f3179
출처 데이터셋
uspto-grants-2013_06
특허 번호
US08466283B2

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