HuagongsheHuagongshe Chemistry Print Report · For research reference only
Methylboronic Acid → [4-(1,1-Dioxo-1lambda6-isothiazolidin-2-yl)-2-methanesulfonylphenyl][4-(4-methylbenzoyl)piperidin-1-yl]methanone
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Methylboronic Acid | HCID 139377 | — |
| Reactant | [4-(4-Chlorobenzoyl)piperidin-1-yl][4-(1,1-dioxo-1lambda6-isothiazolidin-2-yl)-2-methanesulfonylphenyl]methanone | HCID 71252067 | — |
| Product | [4-(1,1-Dioxo-1lambda6-isothiazolidin-2-yl)-2-methanesulfonylphenyl][4-(4-methylbenzoyl)piperidin-1-yl]methanone | HCID 71252631 | 50.7% |
Reaction Steps
Using 4-(1,1-dioxo-1λ6-isothiazolidin-2-yl)-2-methanesulfonylbenzoic acid (138 mg) described in Preparation Example 22 and 4-(4-chlorobenzoyl)piperidine (97 mg) and by the reaction and treatment in the same manner as in Example 87, [4-(4-chlorobenzoyl)piperidin-1-yl][4-(1,1-dioxo-1λ6-isothiazolidin-2-yl)-2-methanesulfonylphenyl]methanone (76 mg) was obtained. Using the obtained [4-(4-chlorobenzoyl)piperidin-1-yl][4-(1,1-dioxo-1λ6-isothiazolidin-2-yl)-2-methanesulfonylphenyl]methanone (76 mg) and methylboronic acid (37 mg) and by the reaction and treatment in the same manner as in Example 115, the title compound (37 mg) was obtained.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08816079B2 |
| Source dataset | uspto-grants-2014_08 |
| ORD ID | ord-31c50ae43f4f4906af6e680bbf282952 |
| Source note | uspto-grants-2014_08 |