HuagongsheHuagongshe Chemistry Print Report · For research reference only
4-Amino-2-methylpyridine → (RS)-N-(Ethoxycarbonyl)-S-methyl-S-[3-({[4-(2-methyl-4-pyridylamino)-6-methoxyquinazolin-7-yl]oxy}methyl)phenyl]sulphoximide
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 4-Amino-2-methylpyridine | HCID 728670 | — |
| Reactant | N'-(2-cyano-5-{3-[(RS)-N-(ethoxycarbonyl)-S-methylsulphonimidoyl]benzyloxy}-4-methoxyphenyl)-N,N-dimethylformimidamide | HCID 57788001 | — |
| Solvent | Dichloromethane methanol | HCID 21226129 | — |
| Product | (RS)-N-(Ethoxycarbonyl)-S-methyl-S-[3-({[4-(2-methyl-4-pyridylamino)-6-methoxyquinazolin-7-yl]oxy}methyl)phenyl]sulphoximide | HCID 57788005 | 19% |
Reaction Steps
According to GWP 5, the reaction of N′-(2-cyano-5-{3-[(RS)-N-(ethoxycarbonyl)-S-methylsulphonimidoyl]benzyloxy}-4-methoxyphenyl)-N,N-dimethylformimidamide (100 mg, 0.22 mmol) with 4-amino-2-methylpyridine (28 mg, 0.26 mmol) and chromatography (silica gel, dichloromethane/methanol: 4/1) gives the desired product in 19% yield (21 mg).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US07863283B2 |
| Source dataset | uspto-grants-2011_01 |
| ORD ID | ord-6c8e3870158b4dee9da448354d95c353 |
| Source note | uspto-grants-2011_01 |