Morpholine → 4-(2-Amino-pyrimidin-5-yl)-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidine-7-carboxylic acid methyl-(3-morpholin-4-yl-phenyl)-amide

HRID 912316

反応式

HRID 912316 の反応式
Br[C:2]1[CH:3]=[C:4]([N:8]([CH3:51])[C:9]([N:11]2[C:15]3[N:16]=[C:17]([N:45]4[CH2:50][CH2:49][O:48][CH2:47][CH2:46]4)[N:18]=[C:19]([C:20]4[CH:21]=[N:22][C:23]([N:26](CC5C=CC(OC)=CC=5)CC5C=CC(OC)=CC=5)=[N:24][CH:25]=4)[C:14]=3[CH2:13][CH2:12]2)=[O:10])[CH:5]=[CH:6][CH:7]=1.[NH:52]1[CH2:57][CH2:56][O:55][CH2:54][CH2:53]1.N1(C2C=C(NC(N3C4N=C(N5CCOCC5)N=C(C5C=NC(N(CC6C=CC(OC)=CC=6)CC6C=CC(OC)=CC=6)=NC=5)C=4CC3)=O)C=CC=2)CCOCC1>>[CH3:51][N:8]([C:4]1[CH:5]=[CH:6][CH:7]=[C:2]([N:52]2[CH2:57][CH2:56][O:55][CH2:54][CH2:53]2)[CH:3]=1)[C:9]([N:11]1[C:15]2[N:16]=[C:17]([N:45]3[CH2:50][CH2:49][O:48][CH2:47][CH2:46]3)[N:18]=[C:19]([C:20]3[CH:21]=[N:22][C:23]([NH2:26])=[N:24][CH:25]=3)[C:14]=2[CH2:13][CH2:12]1)=[O:10]

参加物

4

反応物 3

HCID 8083MorpholineHCID 592449624-{2-[Bis-(4-methoxy-benzyl)-amino]-pyrimidin-5-yl}-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidine-7-carboxylic acid (3-bromo-phenyl)-methyl-amideHCID 866401304-{2-[Bis-(4-methoxy-benzyl)-amino]-pyrimidin-5-yl}-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidine-7-carboxylic acid (3-morpholin-4-yl-phenyl)-amide

生成物 1

HCID 592445644-(2-Amino-pyrimidin-5-yl)-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidine-7-carboxylic acid methyl-(3-morpholin-4-yl-phenyl)-amide収率 61.3%

実験手順

Using 4-{2-[bis-(4-methoxy-benzyl)-amino]-pyrimidin-5-yl}-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidine-7-carboxylic acid (3-bromo-phenyl)-methyl-amide (112 mg) and morpholine (15.5 mg) instead of 2-piperazin-1-yl-ethanol, in the same manner as Step C in Example 1-D-153, 4-{2-[bis-(4-methoxy-benzyl)-amino]-pyrimidin-5-yl}-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidine-7-carboxylic acid (3-morpholin-4-yl-phenyl)-amide was obtained as a crude product. The PMB groups were removed according to Deprotection method 3, to obtain the desired compound (1-D-226) as a yellow solid (47.3 mg, 61%).

後処理

  1. customThe PMB groups were removed

出典と根拠

ORDレコード
ord-8e1af3675722471791181e49aca32507
出典データセット
uspto-grants-2011_09
特許番号
US08022205B2

関連ノート

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