HuagongsheHuagongshe Chemistry Print Report · For research reference only
1-Hydroxybenzotriazole → 1-(6-methoxy-1-{2-[trans-octahydroisoquinolin-2 (1H)-yl]-2-oxoethyl}-1H-indazol-3-yl)-2,2-dimethylpropan-1-one
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 1-Hydroxybenzotriazole | HCID 75771 | — |
| Reactant | Diisopropylethylamine | HCID 81531 | — |
| Reactant | trans-Decahydroisoquinoline | HCID 11083964 | — |
| Reactant | [3-(2,2-Dimethylpropanoyl)-6-methoxy-1H-indazol-1-yl]acetic acid | HCID 57675531 | — |
| Solvent | 1,2-Dichloroethane | HCID 11 | — |
| Solvent | Dimethylformamide | HCID 6228 | — |
| Product | 1-(6-methoxy-1-{2-[trans-octahydroisoquinolin-2 (1H)-yl]-2-oxoethyl}-1H-indazol-3-yl)-2,2-dimethylpropan-1-one | HCID 10386937 | — |
Reaction Steps
To a solution of 29.0 mg [3-(2,2-dimethylpropanoyl)-6-methoxy-1H-indazol-1-yl]acetic acid in 1 mL DMF was added 23.0 mg HOBt, 20.9 mg trans-decahydroisoquinoline, 38.3 mg EDC, and 45.2 mg DIEA in that order. The mixture was stirred at room temperature over night and purified by RP-HPLC using 65-100% MeCN gradient. The pure product fractions were pooled and lyophilized to give the title compound. LC-MS: 4.29 min. (m/Z=412.3, 434.3).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US07528163B2 |
| Source dataset | uspto-grants-2009_05 |
| ORD ID | ord-bd375311500a4842a5d0d62c0fd11f70 |
| Source note | uspto-grants-2009_05 |