On August 18, 2016, Albrecht, Brian K.; Gehling, Victor C.; Harmange, Jean-Christophe; Vaswani, Rishi G. published a patent.Category: indole-building-block The title of the patent was Preparation of substituted indolecarboxamides as modulators of methyl modifying enzymes. And the patent contained the following:
The title compounds I [R1 = alkyl, alkoxy, or OCHF2; R2 = H, Me, Et, thiazolyl, etc.; R3, R31, R4, R41 = H, CF3, Me, Et, etc. (provided that at least one of R3, R31, R4 and R41 is not H); or R3 and R4 or R31 and R41 are taken together form a Ph or cyclohexyl ring], useful for treating a variety of diseases, disorders or conditions associated with Me modifying enzymes, notably EZH1 and EZH2, were prepared E.g., a multi-step synthesis of II, starting from Me 2-methyl-1-[1-(1-methyl-2-oxopiperidin-4- yl)ethyl]-1H-indole-3-carboxylate, was described. Exemplified compounds I were tested for their EZH2 activity (data given). Also provided are pharmaceutical compositions comprising compounds I, pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with Me modifying enzymes, such as cancer. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Category: indole-building-block
The Article related to indolecarboxamide pyridinylmethyl preparation modulator methyl modifying enzyme ezh1 ezh2, antitumor indolecarboxamide pyridinylmethyl preparation ezh1 ezh2 modulator, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Category: indole-building-block
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles