C07B2200/07

METHODS FOR CHIRAL RESOLUTION OF TROLOX

The invention relates to methods of separating Trolox isomers (R)-Trolox and (S)-Trolox, comprising: (a) contacting a mixture of (R) and (S)-Trolox with a resolving agent selected from the group consisting of (1S,2S)-(+)-Pseudoephedrine, (R)-(+)-2-Amino-3-phenyl-1-propanol, (1R,2R)-(−)-Pseudoephedrine, and (S)-(−)-2-Amino-3-phenyl-1-propanol, wherein the resolving agent forms a solid salt with one of (R)-Trolox and (S)-Trolox, and substantially does not form a solid salt with the other; and (b) separating the solid salt from the Trolox isomer that did not form the solid salt with the resolving agent.

SALTS OF AZA-BICYCLIC DI-ARYL ETHERS AND METHODS TO MAKE THEM OR THEIR PRECURSORS

The present invention relates to salts of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane, to methods for making them or their precursors, to pharmaceutical compositions comprising them, and to their use as medicaments.

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”).

##STR00001##

METHOD FOR PRODUCING PROTON PUMP INHIBITOR COMPOUND HAVING OPTICAL ACTIVITY

A highly pure optically active proton pump inhibitor compound can be produced safely and inexpensively in a high yield and enantioselectivity by a method of producing an optically active sulfoxide of Formula 2 or a salt thereof, comprising oxidizing a sulfide of Formula 1 or a salt thereof with hydrogen peroxide using an iron salt in the presence of a chiral ligand of Formula 3; wherein A is CH or N; R.sup.1 is hydrogen atom, an alkyl optionally substituted by halogen(s), or an alkoxy optionally substituted by halogen(s); one to three R.sup.2 may exist, and each of R.sup.2 is independently an alkyl, a dialkylamino, or an alkoxy optionally substituted by halogen(s) or alkoxy(s); each of R.sup.3 is independently hydrogen atom, a halogen, cyano or the like; R.sup.4 is a tertiary alkyl; and * and ** represent respectively R configuration or S configuration.

##STR00001##

Protease inhibitors for treatment of coronavirus infections

Provided herein are compounds of Formula (I), their pharmaceutically acceptable salts, and their pharmaceutical compositions: ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4, R.sup.5, and A are defined in the present disclosure. The compounds are potent inhibitors of the main protease (M.sup.pro) of severe acute respiratory syndrome Coronavirus-2 (SARS-CoV-2), and they are useful in treating or preventing COVID-19 in a subject.

NOVEL COMPOUND USEFUL AS TOLL-LIKE RECEPTOR 7 ACTIVATION INHIBITOR

CB-7 exhibits a weak TLR7 inhibiting effect in normal mice. The present invention provides a novel compound with a stronger TLR7 inhibiting effect than CB-7, a pharmaceutically acceptable salt of said compound, or a prodrug of said compound or salt. The present invention also provides a drug for the prevention or treatment of diseases associated with the activation of TLR7, said drug including the aforementioned TLR7 activation inhibitor.

ACC INHIBITOR AND USE THEREOF

The present invention provides a compound suitable for use as an acetyl CoA carboxylase (ACC) inhibitor, specifically, a thienopyridine derivative, and use of the compound in the preparation of drugs for treating metabolic disorders, cancers or other proliferative disorders, and nonalcoholic steatohepatitis (NASH).

LEFT-HANDED BICYCLIC MORPHOLINE AND SALT THEREOF, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION, AND USE

The invention relates to the field of pharmaceutical chemistry, and it particularly relates to a left-handed bicyclic morpholine and a pharmaceutically acceptable salt thereof, a preparation method therefor, a pharmaceutical composition and use thereof in the preparation of medicaments for preventing and/or treating liver diseases and the like.

CONVERSION OF THC, CBD AND THEIR DERIVATIVES TO CANNABINOL

In a method for aromatizing an alicyclic region of a cannabinoid, especially in enantiopure, scalemic and/or racemic form, in particular for aromatizing the cyclohexene group in Δ.sup.9-THC-C.sub.5, Δ.sup.9-THCA-C.sub.5 A, Δ.sup.9-THCV-C.sub.3, Δ.sup.9-THCVA-C.sub.5 A, and/or scalemic or racemic mixtures of these substances, wherein an oxidizing agent is added to the cannabinoid, sulfur is used as the oxidizing agent.

Process for producing (R)-3-hydroxybutyl (R)-3-hydroxybutyrate

Embodiments of the present invention are directed to processes for the production of (R)-3-hydroxybutyl (R)-3-hydroxybyrate. Poly (R)-3-hydroxybyrate is transesterified with an alcohol, to form a first ester portion and a second ester portion. The first ester portion is reduced to the diol to form a diol portion and the diol portion is reacted with the second ester portion to produce (R)-3-hydroxybutyl (R)-3-hydroxybyrate.