Final Thoughts on Chemistry for Ethyl 5-chloro-6-fluoro-1H-indole-2-carboxylate

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, Application In Synthesis of Ethyl 5-chloro-6-fluoro-1H-indole-2-carboxylate, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 473257-60-2, Name is Ethyl 5-chloro-6-fluoro-1H-indole-2-carboxylate, molecular formula is C11H9ClFNO2. In a Article, authors is Branca, Quirico，once mentioned of 473257-60-2

Reversible and selective monoamine oxidase-A inhibitors (RIMA’s) like moclobemide (Aurorix<*>) have rehabilitated the use of MAO inhibitors as drugs of choice in depression.Starting from the structure of moclobemide, we tried to identify novel types of MAO inhibitors by bioisosteric replacement of the amide group. 2-Aminomethyl-5-phenylpyrroles retained some in vitro activity and served as a starting point for the construction of restricted rotation analogues. 3,4-Dihydro-6-phenylpyrrolo<1,2-a>pyrazines were the most interesting members of a family of 6-, 7-, and 8-phenyl-substituted pyrrolo<1,2-a>pyrazines and were subsequently optimized.A ‘lipophilic linker’ between phenyl and pyrrole ring proved exceedingly useful to improve affinity and led to the benzolpyrazino<1,2-a>indole ring system.Synthetic procedures starting from substituted 1-tetralones allowed the synthesis of substituted derivatives of this ring system.Once the optimal substitution pattern had been identified, facile synthesis of derivatives was achieved from aromatic triflates by Stille or Suzuki coupling.In this series selective and reversible monoamine oxidase-A inhibitors as well as mixed MAO-A and B inhibitors were identified.Affinity of these compounds for MAO was in the nanomolar or even sub-nanomolar range (for monoamine oxidase-A).In conclusion, benzopyrazino<1,2-a>indoles have been identified as a new class of reversible and highly potent monoamine oxidase inhibitors.

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Reference：
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