- Preparation method of arbidol intermediate
-
The invention discloses a preparation method of an arbidol intermediate. Ethyl acetoacetate, monomethylamine and p-benzoquinone used as initial raw materials undergo methylation, cyclization, acetylation, bromination and benzene vulcanization to prepare the target compound ethyl 5-hydroxy-6-bromo-2-phenylthiomethyl-1-methylindole-3-carboxylate. The preparation method of the arbidol intermediate issimple and convenient to operate, cheap and easily available in raw materials, high in yield, low in cost, good in quality, environment-friendly, mild in reaction condition, high in safety productioncoefficient and suitable for large-scale industrial production.
- -
-
Paragraph 0022
(2020/07/02)
-
- PYRROLOBENZODIAZEPINE PRODRUGS AND ANTIBODY CONJUGATES THEREOF
-
The invention relates generally to pyrrolobenzodiazepine monomer and dimer prodrugs having a glutathione-activated disulfide prodrug moiety, a DT-diaphorase-activated quinone prodrug moiety or a reactive oxygen species-activated aryl boronic acid or aryl boronic ester prodrug moiety. The invention further relates to pyrrolobenzodiazepine prodrug dimer-antibody conjugates.
- -
-
Page/Page column 177
(2018/03/06)
-
- Ring Cleavage Reactions of 3- and 5-Non-substituted Isoxazoles
-
5-Methylisoxazoles with electron-accepting groups at C-4 (Ia-c) and 2,3-dimethylisoxazolium iodide (II) undergo ring cleavage when treated with organic bases.The nature of the open chain products which were obtained (stable enolates, β-diketones, esters) depends on the group at C-4 and the strength of the base.In some of these processes aromatic aldehydes were used in order to determine the competition between the condensation and the cleavage reaction.The mechanism of the nucleophilic ring cleavage of II is also shown.
- Alberola, A.,Gonzalez, A. M.,Guerra, D.,Pulido, F. J.
-
p. 1073 - 1076
(2007/10/02)
-