Formaldehyde → (S)-4-(2-chloro-7-methyl-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)-3-methylmorpholine

HRID 1626575노트

반응식

HRID 1626575 반응식
[Cl:1][C:2]1[N:3]=[C:4]([N:15]2[CH2:20][CH2:19][O:18][CH2:17][C@@H:16]2[CH3:21])[C:5]2[CH2:10][N:9]([CH2:11][CH:12]3CC3)[CH2:8][C:6]=2[N:7]=1.C=O.Cl.ClC1N=C(N2CCOC[C@@H]2C)C2CCNCC=2N=1>>[Cl:1][C:2]1[N:3]=[C:4]([N:15]2[CH2:20][CH2:19][O:18][CH2:17][C@@H:16]2[CH3:21])[C:5]2[CH2:12][CH2:11][N:9]([CH3:10])[CH2:8][C:6]=2[N:7]=1

참가 물질

4

반응물 3

HCID 712FormaldehydeHCID 86663153(S)-4-(2-chloro-6-(cyclopropylmethyl)-6,7-dihydro-5H-pyrrolo[3,4-d]pyrimidin-4-yl)-3-methylmorpholineHCID 86663157(S)-4-(2-chloro-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)-3-methylmorpholine hydrochloride

생성물 1

HCID 86663156(S)-4-(2-chloro-7-methyl-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)-3-methylmorpholine수율 78%

실험 절차

Method as described for intermediate 8 using formaldehyde (37% solution in water) and (S)-4-(2-chloro-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)-3-methylmorpholine hydrochloride as starting materials. The mixture was partitioned between saturated NaHCO3 solution and DCM. The organic layer was recovered, dried over MgSO4, filtered and reduced in vacuo, yielding the title compound (2.11 g, 7.47 mmol, 78%).

후처리

  1. customThe mixture was partitioned between saturated NaHCO3 solution and DCM
  2. customThe organic layer was recovered
  3. dry with materialdried over MgSO4
  4. filtrationfiltered

출처 및 근거

ORD 기록
ord-4ddc060b4eca455c9fc74846fd6ef09b
출처 데이터셋
uspto-grants-2014_07
특허 번호
US08785457B2

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