HuagongsheHuagongshe Chemistry Print Report · For research reference only
(4S)-6-Azaspiro[2.5]octan-4-ol → (4S)-6-Azaspiro[2.5]octan-4-ol hydrochloride
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | (4S)-6-Azaspiro[2.5]octan-4-ol | HCID 44541813 | — |
| Reactant | 4-[(R)-4-(3-Chloro-4-trifluoromethyl-phenyl)-3-methyl-7-oxo-2,3,4,7-tetrahydro-[1,4]diazepin-1-yl]-butyric acid | HCID 67074785 | — |
| Product | (4S)-6-Azaspiro[2.5]octan-4-ol hydrochloride | HCID 44541812 | — |
Reaction Steps
In analogy to the procedure described in Example 15, 4-[(R)-4-(3-chloro-4-trifluoromethyl-phenyl)-3-methyl-7-oxo-2,3,4,7-tetrahydro-[1,4]diazepin-1-yl]-butyric acid (22% ee) (intermediate 34) and 1.1 eq. of (S)-6-aza-spiro[2.5]octan-4-ol; hydrochloride (intermediate 2) gave after purification by flash chromatography (50 g amine-silica, ethyl acetate/n-heptane 1:1, 4:1, 9:1, 100%, ethyl acetate/ethanol 99:1 to 95:5) 69% of the title compound as off-white foam. MS: 500.19 (MH+, Cl).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08445674B2 |
| Source dataset | uspto-grants-2013_05 |
| ORD ID | ord-1282685e8c4d4ed09d5c71e4ece470f7 |
| Source note | uspto-grants-2013_05 |