Diethyl (3-aminopropyl)phosphonate → Diethyl 3-(4-(1-(2-(Dimethylamino)-6-methoxybenzyl)piperidin-4-ylamino)quinazolin-2-ylamino)propylphosphonate

HRID 215915

반응식

HRID 215915 반응식
Cl[C:2]1[N:11]=[C:10]([NH:12][CH:13]2[CH2:18][CH2:17][N:16]([CH2:19][C:20]3[C:25]([O:26][CH3:27])=[CH:24][CH:23]=[CH:22][C:21]=3[N:28]([CH3:30])[CH3:29])[CH2:15][CH2:14]2)[C:9]2[C:4](=[CH:5][CH:6]=[CH:7][CH:8]=2)[N:3]=1.[NH2:31][CH2:32][CH2:33][CH2:34][P:35](=[O:42])([O:39][CH2:40][CH3:41])[O:36][CH2:37][CH3:38]>CCCCO>[CH3:29][N:28]([CH3:30])[C:21]1[CH:22]=[CH:23][CH:24]=[C:25]([O:26][CH3:27])[C:20]=1[CH2:19][N:16]1[CH2:17][CH2:18][CH:13]([NH:12][C:10]2[C:9]3[C:4](=[CH:5][CH:6]=[CH:7][CH:8]=3)[N:3]=[C:2]([NH:31][CH2:32][CH2:33][CH2:34][P:35](=[O:42])([O:36][CH2:37][CH3:38])[O:39][CH2:40][CH3:41])[N:11]=2)[CH2:14][CH2:15]1

참가 물질

4

반응물 2

HCID 78113Diethyl (3-aminopropyl)phosphonateHCID 580062552-Chloro-N-(1-(2-(dimethylamino)-6-methoxybenzyl)piperidin-4-yl)quinazolin-4-amine

생성물 1

HCID 58006204Diethyl 3-(4-(1-(2-(Dimethylamino)-6-methoxybenzyl)piperidin-4-ylamino)quinazolin-2-ylamino)propylphosphonate

시약·촉매·용매 1

HCID 2631-Butanol용매

반응 조건

온도
117 °C

실험 절차

Following General Procedure D, Compound 47 (50 mg, 0.12 mmol) and diethyl 3-aminopropylphosphonate (69 mg, 0.36 mmol) in n-BuOH (3 mL) were heated to 117° C. for 24 h with a reflux condenser. The product (Compound 81) was purified by preparative silica gel TLC plate 1000μ using 5% (7N NH3-MeOH) and 95% CH2Cl2 solution as eluent.

후처리

  1. customThe product (Compound 81) was purified by preparative silica gel TLC plate

출처 및 근거

ORD 기록
ord-ce4843057c1b49bcb9d1098f304d04c1
출처 데이터셋
uspto-grants-2012_06
특허 번호
US08193203B2

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