HuagongsheHuagongshe Chemistry Print Report · For research reference only
1,4,5,6-Tetrahydropyrimidin-2-amine → (1,1-dimethyl ethyl) N-(5-bromo-2-benzoxazolyl)-3-[[4-[3-oxo-3-[(1,4,5,6-tetrahydro-2-pyrimidinyl)amino]propyl]benzoyl]amino]-L-alaninate
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 1,4,5,6-Tetrahydropyrimidin-2-amine | HCID 3287412 | — |
| Reactant | (1,1-dimethyl ethyl) N-(5-bromo-2-benzoxazolyl)-3-[[4-(3-methoxy-3-oxo-propyl)benzoyl]amino]-L-alaninate | HCID 69733400 | — |
| Solvent | Tetrahydrofuran | HCID 8028 | — |
| Product | (1,1-dimethyl ethyl) N-(5-bromo-2-benzoxazolyl)-3-[[4-[3-oxo-3-[(1,4,5,6-tetrahydro-2-pyrimidinyl)amino]propyl]benzoyl]amino]-L-alaninate | HCID 69733401 | 45.2% |
Reaction Steps
1,4,5,6-tetrahydro-2-pyrimidinamine (94 mg) is added to the ester 10-6 (140 mg) in 3 ml of THF, and agitation is carried out at ambient temperature for 4 hours. After evaporating under reduced pressure, the dry extract obtained is purified by chromatography eluting with a CH2Cl2/AcOEt 80/20 then CH2Cl2/MeOH 85/15 mixture. 71 mg of expected product 10-7 is obtained.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US06838453B2 |
| Source dataset | uspto-grants-2005_01 |
| ORD ID | ord-24e7fed304634e6a97f2af293897ddfd |
| Source note | uspto-grants-2005_01 |