186498-29-3

Upstream product

• 547-63-7 Methyl isobutyrate 
• 589-15-1 1-bromomethyl-4-bromobenzene 

Downstream Products

• 1613145-95-1 3-(4-bromobenzyl)-3-methyl-1-(quinolin-8-yl)azetidin-2-one 
• 1613146-02-3 4-(4-bromophenyl)-3,3-dimethyl-1-(8-quinolinyl)-2-azetidinone 
• 1429896-55-8 3-(4-bromophenyl)-2,2-dimethyl-N-(quinolin-8-yl)propanamide 
• 1429896-41-2 2-(4-bromobenzyl)-3-(4-methoxyphenyl)-2-methyl-N-(quinolin-8-yl)propanamide 
• 186498-30-6 1-bromo-4-(2-carboxy-2-methylpropyl)benzene 
• 223555-27-9 methyl 2,2-dimethyl-3-(4-tributylstannylphenyl)propionate 

Relevant academic research and scientific papers

DIHYDROPYRIMIDINE COMPOUNDS AND USES THEREOF IN MEDICINE

Provided herein are a dihydropyrimidine compound and use as a medicament, especially application as a medicament used for treating and preventing hepatitis B. Specifically, provided herein is a compound having Formula (I) or (Ia), or a stereisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, wherein the variables of the formulas are as defined in the specification. Also provided herein is use of the compound having Formula (I) or (Ia), or an enantiomer, a diastereoisomer, a tautomer, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof as a medicament, especially use as a medicament for treating and preventing hepatitis B.

Dihydropyridine compound and application thereof to drugs

The invention relates to a dihydropyridine compound and application of the dihydropyridine compound serving as a drug, in particular to application of the dihydropyridine compound serving as a drug for treating and preventing hepatitis B. Specifically, the invention relates to the compound shown as the general formula (I) or (Ia) (please see the specifications for the general formula (I) or (Ia))or stereoisomers, tautomer, a nitrogen oxide, solvate, metabolites and medically acceptable salt of the compound or a prodrug of the compound, wherein all variables are defined in the specification. The invention further relates to application of the compound shown as the general formula (I) or (Ia) or enantiomers, non-enantiomers, the tautomer, hydrates, the solvate or the medically acceptable salt of the compound serving as drugs, in particular to application of the compound or the enantiomers, the non-enantiomers, the tautomer, the hydrates, the solvate or the medically acceptable salt of the compound serving as the drugs for treating and preventing hepatitis B.

Copper-catalyzed intramolecular C(sp3)-H and C(sp2)-H amidation by oxidative cyclization

The first copper-catalyzed intramolecular C(sp3)-H and C(sp 2)-H oxidative amidation has been developed. Using a Cu(OAc) 2 catalyst and an Ag2CO3 oxidant in dichloroethane solvent, C(sp3)-H

β-Arylation of carboxamides via iron-catalyzed C(sp3)-H bond activation

A 2,2-disubstituted propionamide bearing an 8-aminoquinolinyl group as the amide moiety can be arylated at the β-methyl position with an organozinc reagent in the presence of an organic oxidant, a catalytic amount of an iron salt, and a biphosphine ligand at 50 C. Various features of selectivity and reactivity suggest the formation of an organometallic intermediate via rate-determining C-H bond cleavage rather than a free-radical-type reaction pathway.

Pd(II)-catalyzed primary-C(sp3)-H acyloxylation at room temperature

With the aid of a novel S-methyl-S-2-pyridyl-sulfoximine (MPyS) directing group (DG), the unactivated primary β-C(sp3)-H bond of MPyS-N-amides oxidizes at room temperature. The catalytic conditions are applicable to the diacetoxylation of primary β,β′-C(sp 3)-H bonds, and the carboxylic acid solvent is pivotal in the formation of the C-O bond. The MPyS-DG cleaves from the oxidation products and is recovered. This method provides convenient access to α,α′- disubstituted-β-hydroxycarboxylic acids.

Heterocyclic compounds

The invention concerns pharmaceutically useful compounds of the formula I, in which A1, A2, A3, A4, B1, m, Ar, W, X, Y, Z and R1 have any of the meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.

N-heterocyclic sulfonamides having endothelin receptor activity

The invention concerns pharmaceutically useful compounds of the formula I, in which R 1, R 2, R 3, n, m and Het have any of the meanings defined herein, and their pharmaceutically-acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processess for the manufacture of the novel compounds and the use of the compounds in medical treatment.