HuagongsheHuagongshe Chemistry Print Report · For research reference only
(6-Chloro-1-benzothiophen-2-yl)methanol → tert-Butyl (tert-butoxycarbonyl {6-[(6-chlorobenzo[b]thiophen-2-ylmethyl)(pyridin-3-ylsulfonyl)aminomethyl]pyridin-2-yl}amino)acetate
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | (6-Chloro-1-benzothiophen-2-yl)methanol | HCID 36995598 | — |
| Reactant | N-[4-(thiazol-2-yl)benzyl]pyridin-3-ylsulfonamide | HCID 66717376 | — |
| Reactant | Tert-butyl (tert-butoxycarbonyl{6-[(pyridin-3-ylsulfonyl)aminomethyl]pyridin-2-yl}amino)acetate | HCID 86651773 | — |
| Product | tert-Butyl (tert-butoxycarbonyl {6-[(6-chlorobenzo[b]thiophen-2-ylmethyl)(pyridin-3-ylsulfonyl)aminomethyl]pyridin-2-yl}amino)acetate | HCID 86651775 | 104.5% |
Reaction Steps
Reaction and post-treatment were carried out in the same manner as in Example 2-(a) except for using tert-butyl(tert-butoxycarbonyl{6-[(pyridin-3-ylsulfonyl)aminomethyl]pyridin-2-yl}amino)acetate (100 mg, 0.209 mmol) obtained in Reference Example 12-(d) in place of N-[4-(thiazol-2-yl)benzyl]pyridin-3-ylsulfonamide, and using (6-chlorobenzo[b]thiophen-2-yl)methanol (see WO 99/37304A, 41.5 mg, 0.209 mmol) in place of tert-butyl[tert-butoxycarbonyl(6-hydroxymethylpyridin-2-yl)amino]acetate to afford the title compound (144 mg) substantially quantitatively as a slightly yellow liquid.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08648097B2 |
| Source dataset | uspto-grants-2014_02 |
| ORD ID | ord-66a151d21a894c7d9d6c8753a5af0f98 |
| Source note | uspto-grants-2014_02 |