On May 7, 2020, Lee, Matthew Randolph; Varano, Anthony Joseph, Jr. published a patent.Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Sulfonylisoquinolinone derivatives as ROCK kinase inhibitors and their preparation. And the patent contained the following:
The invention relates to compounds of formulas I and II that inhibit ROCK activity. The invention relates to compounds of formulas I and II, pharmaceutical compositions and methods of use, such as methods of inhibiting ROCK activity and methods for treating, for example cerebral cavernous malformation syndrome (CCM) and cardiovascular diseases using the compounds and pharmaceutical compositions of the invention. Compounds of formulas I and II wherein ring X is partially saturated aza-containing heteroaryl; Y is CH and N; m is 0, 1, 2 and 3; each R1 is independently CN, OH, hydroxyalkyl, halo, etc.; R2 is H and halo; R3 is H, halo and C1-3 alkyl; and with provisions; and pharmaceutically acceptable salts thereof, are claimed. Example compound III was prepared by sulfonylation of 1-chloroisoquinoline with chlorosulfonic acid; the resulting 1-chloroisoquinoline-5-sulfonyl chloride underwent hydrolysis to give 1-hydroxyisoquinoline-5-sulfonic acid, which underwent chlorination to give the corresponding sulfonyl chloride, which underwent amidation with 4-methylisoindoline to give compound III. The invention compounds were evaluated for their ROCK kinase inhibitory activity. From the assay, it was determined that compound III exhibited IC50 value in the range of 1,000 nM to ≤ 10,000 nM. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole
The Article related to sulfonylisoquinolinone preparation rock kinase inhibitor, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole
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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