2-Methyl-5-(morpholin-4-ylsulphonyl)benzeneboronic acid → 3-Amino-6-[2-methyl-5-(morpholine-4-sulfonyl)-phenyl]-pyrazine-2-carboxylic acid methoxy-methyl amide

HRID 81479

Reaction equation

HRID 81479 reaction equation
[CH3:1][O:2][N:3]([CH3:21])[C:4]([C:6]1[C:11]([NH2:12])=[N:10][CH:9]=[C:8](C2C=CC(Cl)=C(Cl)C=2)[N:7]=1)=[O:5].[CH3:22][C:23]1[CH:28]=[CH:27][C:26]([S:29]([N:32]2[CH2:37][CH2:36][O:35][CH2:34][CH2:33]2)(=[O:31])=[O:30])=[CH:25][C:24]=1B(O)O>>[CH3:1][O:2][N:3]([CH3:21])[C:4]([C:6]1[C:11]([NH2:12])=[N:10][CH:9]=[C:8]([C:24]2[CH:25]=[C:26]([S:29]([N:32]3[CH2:37][CH2:36][O:35][CH2:34][CH2:33]3)(=[O:31])=[O:30])[CH:27]=[CH:28][C:23]=2[CH3:22])[N:7]=1)=[O:5]

Participants

3

Reactant 2

HCID 441195542-Methyl-5-(morpholin-4-ylsulphonyl)benzeneboronic acidHCID 866345423-Amino-6-(3,4-dichloro-phenyl)-pyrazine-2-carboxylic acid methoxy-methyl amide

Product 1

HCID 866345433-Amino-6-[2-methyl-5-(morpholine-4-sulfonyl)-phenyl]-pyrazine-2-carboxylic acid methoxy-methyl amide

Procedure

This compound is prepared in an analogous manner to intermediate B substituting 3,4 dichlorophenyl boronic acid with 2-methyl-5-(N-morpholinylsulfonyl)phenyl boronic acid in step 2. The title compound is obtained as an off-white solid. [M+H]+ 422.

Sources & evidence

ORD record
ord-9e5889ab11b94bd49176e246e6ed9dbc
Source dataset
uspto-grants-2014_09
Patent number
US08846687B2

Linked notes

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