HuagongsheHuagongshe Chemistry Print Report · For research reference only
2-Aminothiazole → (RS)-N-(ethoxycarbonyl)-S-methyl-S-[3-({[4-(thiazol-2-ylamino)quinazolin-7-yl]amino}methyl)phenyl]sulphoximide
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 2-Aminothiazole | HCID 2155 | — |
| Reactant | Dichloromethane methanol | HCID 21226129 | — |
| Reactant | N'-(2-cyano-5-{3-[(RS)-N-(ethoxycarbonyl)-S-methylsulphonimidoyl]benzylamino}phenyl)-N,N-dimethylformimidamide | HCID 57788040 | — |
| Solvent | Methanol | HCID 887 | — |
| Product | (RS)-N-(ethoxycarbonyl)-S-methyl-S-[3-({[4-(thiazol-2-ylamino)quinazolin-7-yl]amino}methyl)phenyl]sulphoximide | HCID 44197696 | 43% |
Reaction Steps
According to GWP 5, the reaction of N′-(2-cyano-5-{3-[(RS)-N-(ethoxycarbonyl)-S-methylsulphonimidoyl]benzylamino}phenyl)-N,N-dimethylformimidamide (90 mg, 0.21 mmol) with 2-aminothiazole (26 mg, 0.25 mmol) and chromatographic purification (silica gel, dichloromethane/methanol: 0→30% methanol) gives the desired product in 43% yield (43 mg).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US07863283B2 |
| Source dataset | uspto-grants-2011_01 |
| ORD ID | ord-621789a39ea5407cb0fccd0f799aaa4a |
| Source note | uspto-grants-2011_01 |