C07D279/06

S-OXIDES OF 2,3-DIARYL-2,3-DIHYDRO-4H-1,3-THIAZIN-4-ONES AND 2,3-DIARYL-1,3-THIAZEPAN-4-ONES AND METHODS FOR MAKING
20220259165 · 2022-08-18 ·

A compound with the following general formula and a general method of making this compound are provided: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 are each independently selected from the group that includes hydrogen, halogen, nitro, cyano, amido, pyridyl, alkyl, aryl, alkoxy, cycloalkyl, heteroalkyl, heterocyclyl, aralkyl, heteroaryl and heteroaralkyl.

##STR00001##

S-OXIDES OF 2,3-DIARYL-2,3-DIHYDRO-4H-1,3-THIAZIN-4-ONES AND 2,3-DIARYL-1,3-THIAZEPAN-4-ONES AND METHODS FOR MAKING
20220259165 · 2022-08-18 ·

A compound with the following general formula and a general method of making this compound are provided: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 are each independently selected from the group that includes hydrogen, halogen, nitro, cyano, amido, pyridyl, alkyl, aryl, alkoxy, cycloalkyl, heteroalkyl, heterocyclyl, aralkyl, heteroaryl and heteroaralkyl.

##STR00001##

Processes to produce elagolix

The present invention relates to a scalable process for the making of elagolix, its salts and the process of intermediate compounds.

CF3-, OCF3-, SCF3-, and SF5-Containing Antibacterial Agents
20220249447 · 2022-08-11 ·

The present invention generally relates to compounds as a new antibiotic to treat various infections, including infections caused by methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-intermediate and vancomycin-resistant S. aureus (VISA and VRSA respectively) vancomycin-resistant Enterococcusfaecalis (VRE), and Clostridioides difficile. Pharmaceutical compositions and methods for treating those infection diseases are within the scope of this invention.

2,3-Diaryl-2,3-Dihydro-4H-1,3-Thiazin-4-One Compounds and Methods for Making

A compound with the following general formula (I) and a general method of making this compound are provided. R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 are each independently selected from the group that includes H, halogen, nitro, cyano, amido, pyridyl, alkyl, aryl, acyl, alkoxy, cycloalkyl, heteroalkyl, heterocyclyl, aralkyl, heteroaryl and heteroaralkyl.

##STR00001##

2,3-Diaryl-2,3-Dihydro-4H-1,3-Thiazin-4-One Compounds and Methods for Making

A compound with the following general formula (I) and a general method of making this compound are provided. R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 are each independently selected from the group that includes H, halogen, nitro, cyano, amido, pyridyl, alkyl, aryl, acyl, alkoxy, cycloalkyl, heteroalkyl, heterocyclyl, aralkyl, heteroaryl and heteroaralkyl.

##STR00001##

Full continuous-flow preparation method of vitamin B1

A full continuous-flow preparation method of vitamin B.sub.1 includes: (S1) feeding 3-chloro-4-oxopentyl acetate, 2-methyl-4-amino-5-(aminomethyl) pyrimidine and carbon disulfide to a first continuous-flow reactor for addition; (S2) allowing the reaction mixture to flow into a first continuous filtration and reaction device to collect a filter cake; subjecting the filter cake and hydrochloric acid solution to cyclization; transporting the reaction mixture and an aqueous inorganic base solution to a micromixer and a second continuous-flow reactor for hydrolysis to obtain thiothiamine; (S3) transporting the thiothiamine to a third continuous-flow reactor with hydrogen peroxide for oxidation to obtain thiamine sulfate; and (S4) allowing the thiamine sulfate to enter a second continuous filtration and reaction device for filtration to collect a filter cake; and subjecting the filter cake to reaction with organic hydrochloric acid solution followed by filtration and drying to obtain vitamin B.sub.1.

Full continuous-flow preparation method of vitamin B1

A full continuous-flow preparation method of vitamin B.sub.1 includes: (S1) feeding 3-chloro-4-oxopentyl acetate, 2-methyl-4-amino-5-(aminomethyl) pyrimidine and carbon disulfide to a first continuous-flow reactor for addition; (S2) allowing the reaction mixture to flow into a first continuous filtration and reaction device to collect a filter cake; subjecting the filter cake and hydrochloric acid solution to cyclization; transporting the reaction mixture and an aqueous inorganic base solution to a micromixer and a second continuous-flow reactor for hydrolysis to obtain thiothiamine; (S3) transporting the thiothiamine to a third continuous-flow reactor with hydrogen peroxide for oxidation to obtain thiamine sulfate; and (S4) allowing the thiamine sulfate to enter a second continuous filtration and reaction device for filtration to collect a filter cake; and subjecting the filter cake to reaction with organic hydrochloric acid solution followed by filtration and drying to obtain vitamin B.sub.1.

ANTIMICROBIAL COMPOUNDS AND COMPOSITIONS COMPRISING SAME
20220055997 · 2022-02-24 ·

The present invention is directed to antibacterial compositions and methods of use thereof, such as in the treatment of infectious diseases. Additionally, provided herein a method of screening molecules for identifying potential biologically active compounds.

ALPHA-5 BETA-1 INHIBITORS

The disclosure provides, inter alia, alpha-5 beta-1 inhibitors, pharmaceutical compositions comprising alpha-5 beta-1 inhibitors, methods for treating diseases using alpha-5 beta-1 inhibitors, and processes for making alpha-5 beta-1 inhibitors.