Ethyl isocyanate → (S)-1-ethyl-3-(5-(7-methyl-4-(3-methylmorpholino)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)thiazol-2-yl)urea

HRID 1626618노트

반응식

HRID 1626618 반응식
[CH3:1][N:2]1[CH2:11][CH2:10][C:9]2[C:8]([N:12]3[CH2:17][CH2:16][O:15][CH2:14][C@@H:13]3[CH3:18])=[N:7][C:6]([C:19]3[S:23][C:22]([NH2:24])=[N:21][CH:20]=3)=[N:5][C:4]=2[CH2:3]1.[CH2:25]([N:27]=[C:28]=[O:29])[CH3:26]>>[CH2:25]([NH:27][C:28]([NH:24][C:22]1[S:23][C:19]([C:6]2[N:7]=[C:8]([N:12]3[CH2:17][CH2:16][O:15][CH2:14][C@@H:13]3[CH3:18])[C:9]3[CH2:10][CH2:11][N:2]([CH3:1])[CH2:3][C:4]=3[N:5]=2)=[CH:20][N:21]=1)=[O:29])[CH3:26]

참가 물질

3

반응물 2

HCID 8022Ethyl isocyanateHCID 86663160(S)-5-(7-methyl-4-(3-methylmorpholino)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)thiazol-2-amine

생성물 1

HCID 86663161(S)-1-ethyl-3-(5-(7-methyl-4-(3-methylmorpholino)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)thiazol-2-yl)urea수율 11%

실험 절차

The product from step 1 was treated as described for example 85 with ethyl isocyanate. The mixture was concentrated in vacuo and the material purified by prep HPLC at high and low pH, yielding the title compound (15.5 mg, 0.037 mmol, 11% over 2 steps).

후처리

  1. concentrationThe mixture was concentrated in vacuo
  2. customthe material purified by prep HPLC at high and low pH

출처 및 근거

ORD 기록
ord-2f21ae71f13e46b9ad27e965921d8aab
출처 데이터셋
uspto-grants-2014_07
특허 번호
US08785457B2

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