142144-65-8

Upstream product

• 36282-40-3 (3-methoxyphenyl)magnesium bromide 
• 120-92-3 cyclopentanone 
• 2398-37-0 3-methoxyphenyl bromide 

Downstream Products

• 1011361-36-6 1-(3-methoxyphenyl)cyclopentan-1-amine 
• 31503-28-3 (±)-2-(3-methoxyphenyl)cyclopentan-1-one 
• 288591-15-1 {(2R,6S)-6-[3-(tert-Butyl-dimethyl-silanyloxy)-phenyl]-tetrahydro-pyran-2-yl}-acetic acid methyl ester 
• 288591-14-0 (E)-(S)-7-[3-(tert-Butyl-dimethyl-silanyloxy)-phenyl]-7-hydroxy-hept-2-enoic acid methyl ester 
• 288591-02-6 7-[3-(tert-butyl-dimethyl-silanyloxy)-phenyl]-7-oxo-hept-2-enoic acid methyl ester 

Relevant academic research and scientific papers

Synthesis of 4H-1,3-Benzoxazines via Metal- and Oxidizing Reagent-Free Aromatic C-H Oxygenation

An unprecedented electrochemical aromatic C-H oxygenation reaction for the synthesis of 4H-1,3-benzoxazines from easily available N-benzylamides is reported. These oxidative cyclization reactions proceed in a transition metal- and oxidizing reagent-free fashion and produce H2 as only theoretical byproduct. Adapting the C-H oxygenation reaction in an electrochemical microreactor has been demonstrated.

BACE-2 INHIBITORY COMPOUNDS AND RELATED METHODS OF USE

Provided herein are novel compounds of Formulae I-III, and methods of using the same to selectively inhibit BACE2.

Synthesis and in Vitro Anticancer Activity of the First Class of Dual Inhibitors of REV-ERBβ and Autophagy

Autophagy inhibition is emerging as a promising anticancer strategy. We recently reported that the circadian nuclear receptor REV-ERBβ plays an unexpected role in sustaining cancer cell survival when the autophagy flux is compromised. We also identified 4-[[[1-(2-fluorophenyl)cyclopentyl]amino]methyl]-2-[(4-methylpiperazin-1-yl)methyl]phenol, 1 (ARN5187), as a novel dual inhibitor of REV-ERBβ and autophagy. 1 had improved cytotoxicity against BT-474 breast cancer cells compared to chloroquine, a clinically relevant autophagy inhibitor. Here, we present the results of structure-activity studies, based around 1, that disclose the first class of dual inhibitors of REV-ERBβ and autophagy. This study led to identification of 18 and 28, which were more effective REV-ERBβ antagonists than 1 and were more cytotoxic to BT-474. The combination of optimal chemical and structural moieties of these analogs generated 30, which elicited 15-fold greater REV-ERBβ inhibitory and cytotoxic activities compared to 1. Furthermore, 30 induced death in a panel of tumor cell lines at doses 5-50 times lower than an equitoxic amount of chloroquine but did not affect the viability of normal mammary epithelial cells.

DIARYLALKYLAMINE REV-ERB ANTAGONISTS AND THEIR USE AS MEDICAMENTS

The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof : It further discloses a pharmaceutical composition comprising the compounds of Formula (I) and their uses as anti-proliferative and pro-apoptotic agents for cancer therapy.

Regio- and enantioselective Baeyer-Villiger oxidation: Kinetic resolution of racemic 2-substituted cyclopentanones

A kinetic resolution of racemic 2-substituted cyclopentanones via highly regio- and enantioselective Baeyer-Villiger oxidation has been successfully developed. The reaction could afford the normal 6-substituted δ-lactones in up to 98% ee and >19/1 regioselectivity. Meanwhile, the unreacted ketones were recovered in excellent ee values (up to 98%). It represents the best results of the kinetic resolution of racemic 2-substituted cyclopentanones via nonenzymic asymmetric BV oxidation.

Synthesis of simplified herboxidiene aromatic hybrids

The syntheses of simplified aromatic hybrids of the novel polyketide herboxidiene (1) are described. One of the hybrids prepared showed significant herbicidal activity against broad-leaved weeds in post-emergent application. (C) 2000 Elsevier Science Ltd. All rights reserved.