135335-11-4

Upstream product

• 73918-56-6 4-Bromophenethylamine 
• 541-41-3 chloroformic acid ethyl ester 
• 16532-79-9 4-Bromophenylacetonitrile 

Downstream Products

• 258515-65-0 7-bromo-3,4-dihydroisoquinoline-2(1H)-carboxylic acid tert-butyl ester 
• 891782-60-8 7-bromo-3,4-dihydroisoquinolin-1(2 H)-one 
• 17680-55-6 7-bromo-1,2,3,4-tetrahydroisoquinoline 

Relevant academic research and scientific papers

Catalyst-free cyclization of anthranils and cyclic amines: One-step synthesis of rutaecarpine

An efficient synthesis of a variety of quinazolinone derivatives via a direct cyclization reaction between commercially available anthranils and cyclic amines is described. The developed transformation proceeds with the merits of high step- and atom-efficiency, a broad substrate scope, and good to excellent yields, without additional catalysts, and offers a practical way for the preparation of rutaecarpine and its derivatives with structural diversity.

GPR40 receptor stimulant, and preparation method, pharmaceutical composition and application thereof

The invention discloses a GPR40 receptor stimulant, and a preparation method, a pharmaceutical composition and application thereof. The invention particularly discloses a GPR40 receptor stimulant shown in general formula (I) and pharmacologically acceptable salt thereof, a preparation process of the compound, a pharmaceutical composition containing the compound of general formula (I), and application of the compound and the pharmaceutical composition in anti-diabetes.

Design, synthesis and biological evaluation of a series of novel GPR40 agonists containing nitrogen heterocyclic rings

A novel series of GPR40 agonists is designed by introducing nitrogen-containing heterocyclic ring at the terminal phenyl ring of TAK-875 with the aim of decreasing its lipophilicity. Three different β-substituted phenylpropionic acids were investigated as the acidic components. A total of 34 compounds have been synthesized, among which, compound 30 exhibited comparable GPR40 agonistic activity in vitro with TAK-875 and relatively lower lipophilicity through calculation (30, EC50 = 1.2 μM, cLogP = 1.3; TAK-875: EC50 = 5.1 μM, cLogP = 3.4). Moreover, compound 30 was able to enhance the insulin secretion of primary islets isolated from normal ICR mice and showed no obvious inhibition against cytochromes P450 in vitro. In vivo, compound 30 exhibited efficacy in oral glucose tolerance test (oGTT) in normal ICR mice.

17a-HYDROXYLASE/C17,20-LYASE INHIBITORS

The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.

USE OF ARYL CARBAMATES IN AGRICULTURE AND OTHER PLANT-RELATED AREAS

Disclosure is provided for methods of preventing, removing or inhibiting microbial biofilm formation or microbial infection in a plant or plant part thereof, including applying thereto a treatment effective amount of an aryl carbamate as described herein,

INHIBITION OF BACTERIAL BIOFILMS WITH ARYL CARBAMATES

Disclosure is provided for carbamate compounds that prevent, remove and/or inhibit the formation of biofilms, compositions including these compounds, devices including these compounds, and methods of using the same.

USE OF ARYL CARBAMATES IN AGRICULTURE AND OTHER PLANT-RELATED AREAS

Disclosure is provided for methods of preventing, removing or inhibiting microbial biofilm formation or microbial infection in a plant or plant part thereof, including applying thereto a treatment effective amount of an aryl carbamate as described herein,

17α-HYDROXYLASE/C17,20-LYASE INHIBITORS

The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.

Generation of N-Methyl-D-aspartate Agonist and Competitive Antagonist Pharmacophore Models. Design and Synthesis of Phosphonoalkyl-Substituted Tetrahydroisoquinolines as Novel Antagonists

The preparation and binding affinity of a series of tetrahydroisoquinoline carboxylic acids at the N-methyl-D-aspartate (NMDA) subtype of the glutamate receptor is described, together with a molecular modeling analysis of NMDA agonists and antagonists.Usi

Substituted carboxytetrahydroisoquinolines and derivatives thereof having pharmaceutical activity

The invention includes a novel series of substituted aryl or heteroaryl fused 2- or 6-carboxy piperidines and derivatives thereof which are useful in the treatment of cerebrovascular disorders, epilepsy, Huntington's disease, or as anesthetics particularly in surgical processes where a finite risk of cerebrovascular damage exists. Processes for making the compounds, novel intermediates useful in the processes, methods for using, and compositions containing the compounds are also included.