Butane-2-sulphonic acid 5-(2,4-diamino-pyrimidin-5-ylmethyl)-3-ethoxy-2-iodo-phenyl ester → Butane-2-sulphonic acid 3'-amino-4-(2,4-diamino-pyrimidin-5-ylmethyl)-6-ethoxy-4'-morpholin-4-ylmethyl-biphenyl-2-yl ester

HRID 2416329Notes

Reaction equation

HRID 2416329 reaction equation
Br[C:2]1[CH:3]=[CH:4][C:5]([CH2:15][N:16]2[CH2:21][CH2:20][O:19][CH2:18][CH2:17]2)=[C:6]([NH:8]C(=O)C(F)(F)F)[CH:7]=1.[NH2:22][C:23]1[N:28]=[C:27]([NH2:29])[C:26]([CH2:30][C:31]2[CH:32]=[C:33]([O:46][CH2:47][CH3:48])[C:34](I)=[C:35]([O:37][S:38]([CH:41]([CH2:43][CH3:44])[CH3:42])(=[O:40])=[O:39])[CH:36]=2)=[CH:25][N:24]=1>>[NH2:8][C:6]1[CH:7]=[C:2]([C:34]2[C:33]([O:46][CH2:47][CH3:48])=[CH:32][C:31]([CH2:30][C:26]3[C:27]([NH2:29])=[N:28][C:23]([NH2:22])=[N:24][CH:25]=3)=[CH:36][C:35]=2[O:37][S:38]([CH:41]([CH2:43][CH3:44])[CH3:42])(=[O:39])=[O:40])[CH:3]=[CH:4][C:5]=1[CH2:15][N:16]1[CH2:17][CH2:18][O:19][CH2:20][CH2:21]1

Participants

3

Reactant 2

HCID 17937260Butane-2-sulphonic acid 5-(2,4-diamino-pyrimidin-5-ylmethyl)-3-ethoxy-2-iodo-phenyl esterHCID 22636976N-(5-bromo-2-morpholin-4-ylmethyl-phenyl)-2,2,2-trifluoro-acetamide

Product 1

HCID 17937331Butane-2-sulphonic acid 3'-amino-4-(2,4-diamino-pyrimidin-5-ylmethyl)-6-ethoxy-4'-morpholin-4-ylmethyl-biphenyl-2-yl esterYield 57.7%

Procedure

Starting from 308 mg (0.84 mmol) N-(5-bromo-2-morpholin-4-ylmethyl-phenyl)-2,2,2-trifluoro-acetamide and 214 mg (0.422 mmol) butane-2-sulphonic acid 5-(2,4-diamino-pyrimidin-5-ylmethyl)-3-ethoxy-2-iodo-phenyl ester, 139 mg of the title compound are obtained as pale brown crystals.

Sources & evidence

ORD record
ord-3546528182e14c8f91a61fb598e99169
Source dataset
uspto-grants-2004_11
Patent number
US06821980B1

Reaction notes

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