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Disiloxane → 3-[5-(4-Chlorophenyl)pyridin-2-yl]propynoic acid-[4-(4-hydroxypiperidin-1-ylmethyl)phenyl]amide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Disiloxane | HCID 123318 | — |
| 反応物 | Tetrabutylammonium Fluoride | HCID 2724141 | — |
| 反応物 | Ammonia methanol dichloromethane | HCID 21584172 | — |
| 反応物 | [5-(4-chlorophenyl)pyridin-2-yl]propynoic Acid | HCID 68816808 | — |
| 反応物 | 4-[4-(Tert-butyldimethylsilanyloxy)piperidin-1-ylmethyl]phenylamine | HCID 68816909 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | 3-[5-(4-Chlorophenyl)pyridin-2-yl]propynoic acid-[4-(4-hydroxypiperidin-1-ylmethyl)phenyl]amide | HCID 57845715 | — |
反応手順
Prepared analogously to Example 2.3.f. from [5-(4-chlorophenyl)pyridin-2-yl]propynoic acid and 4-[4-(tert-butyldimethylsilanyloxy)piperidin-1-ylmethyl]phenylamine. The cleaving of the silyl group is carried out by adding tetrabutylammonium fluoride to a solution of the silylether in THF. Yield: 0.25 g (43% of theory); melting point: 186° C.-190° C.; C26H24ClN3O2 (M=445.94); calc.: molecular ion peak (M+H)+: 446/448; found: molecular ion peak (M+H)+: 446/448; Rf value: 0.6 (silica gel, dichloromethane/methanol/ammonia (90:10:0.1)).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07592373B2 |
| 出典データセット | uspto-grants-2009_09 |
| ORD ID | ord-4cbfe1198961458581a58cc1efc62848 |
| 出典メモ | uspto-grants-2009_09 |