HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 241877Generated: October 31, 2026
Water → [6-(5-Chloro-pyridin-2-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yl]-[(R)-cyclopropyl-(6-trifluoromethyl-pyridin-3-yl)-methyl]-amine
https://huagongshe.com/reaction/241877
Participants
| Role | Name | HCID | Charge |
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| Reactant | Water | HCID 962 | — |
| Reactant | Diisopropylethylamine | HCID 81531 | — |
| Reactant | 4-Bromo-6-(5-chloropyridin-2-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine | HCID 58103575 | — |
| Reactant | (R)-cyclopropyl(6-(trifluoromethyl)pyridin-3-yl)methanamine dihydrochloride | HCID 66872073 | — |
| Solvent | Acetonitrile | HCID 6342 | — |
| Product | [6-(5-Chloro-pyridin-2-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yl]-[(R)-cyclopropyl-(6-trifluoromethyl-pyridin-3-yl)-methyl]-amine | HCID 25033577 | 30.7% |
Reaction Steps
To a stirred solution of (R)-cyclopropyl(6-(trifluoromethyl)pyridin-3-yl)methanamine dihydrochloride (53 mg, 0.184 mmol) and N,N-diisopropylethylamine (60 uL, 0.4 mmol) in acetonitrile (1.2 mL) was added 4-bromo-6-(5-chloropyridin-2-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine (30 mg, 0.092 mmol). The reaction mixture was heated in microwave reactor at 180° C. for 8 hours. Water was added and the mixture was extracted with ethyl acetate. The organic layers were combined, dried (MgSO4) and concentrated to obtain a brown oil which was purified using HPLC (semi-prep 30-80% water/acetonitrile) to give a light brown solid (13 mg).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08653091B2 |
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| Source dataset | uspto-grants-2014_02 |
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| ORD ID | ord-5093e4ffc178454aa5fcbc39e354989b |
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| Source note | uspto-grants-2014_02 |
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