191731-32-5

Upstream product

• 88920-24-5 p-methoxybenzyloxy acetic acid 
• 6638-79-5 N,O-dimethylhydroxylamine*hydrochloride 
• 67442-07-3 2-chloro-N-methoxy-N-methylacetamide 
• 105-13-5 4-Methoxybenzyl alcohol 

Downstream Products

• 400063-06-1 1-(4-methoxy-benzyloxy)-3-pyridin-4-yl-propan-2-one 
• 482351-08-6 methyl (7R)-α-[[(4-methoxyphenyl)methoxy]acetyl]-1,4-dioxaspiro[4,5]decane-7-acetate 
• 921209-92-9 4-(4-methoxybenzyloxy)-3-oxobutyric acid methyl ester 
• 400063-08-3 2-(4-methoxy-benzyloxymethyl)-6-oxo-1,6-dihydro-[3,4']bipyridinyl-5-carbonitrile 
• 1095223-12-3 1-(2-fluoro-pyridin-3-yl)-2-(4-methoxy-benzyloxy)-ethanone 
• 1159374-12-5 C₁₆H₁₆O₃ 
• 1284219-15-3 6-methoxy-1-phenyl-1H-inden-2(3H)-one 
• 1284219-06-2 C₁₇H₁₅F₃O₅S 
• 1285607-96-6 C₁₆H₁₄O₂ 
• 1434713-46-8 1-((4-methoxybenzyl)oxy)-3-methylbutan-2-one 
• 1600512-80-8 (Z)-N-(1-(5-bromo-2-fluorophenyl)-2-((4-methoxybenzyl)oxy)ethylidene)-2-methylpropane-2-sulfinamide 
• 1600512-81-9 N-(2-(5-bromo-2-fluorophenyl)-1-((2-cyanopropan-2-yl)sulfonyl)-3-((4-methoxybenzyl)oxy)propan-2-yl)-2-methylpropane-2-sulfinamide 
• 1600512-79-5 1-(5-bromo-2-fluorophenyl)-2-((4-methoxybenzyl)oxy)ethanone 

Relevant academic research and scientific papers

Facile KF/alumina mediated synthesis of α-heterosubstituted Weinreb amides

Anhydrous KF/alumina in dipolar aprotic solvents was found to be an effective promoter in the synthesis of α-heterosubstituted Weinreb amides prepared from 2-chloro-N-methoxy-N-methylacetamide. This method is high yielding, even for weak nucleophiles, and

AMINO-DIHYDROTHIAZINE AND AMINO-DIOXIDO DIHYDROTHIAZINE COMPOUNDS AS BETA-SECRETASE ANTAGONISTS AND METHODS OF USE

The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II.

[3,3]-sigmatropic rearrangement/5-exo-dig cyclization reactions of benzyl alkynyl ethers: Synthesis of substituted 2-indanones and indenes

Substituted benzyl alkynyl ethers, prepared from the corresponding α-alkoxy ketones in a two-step sequence involving enol triflate formation and KOtBu-induced E2 elimination, undergo [3,3]-sigmatropic rearrangement/ intramolecular 5-exo-dig cyclization at 60 °C to form substituted 2-indanones in good overall yields. 1,3-cis-Disubstituted-2-indanones are formed preferentially when the benzylic substituent R1 is bulky. Substituted indenes may be prepared from 2-indanones in high yields by Horner-Wadsworth-Emmons reaction.

Expedient synthesis of 3-alkoxymethyl- And 3-aminomethyl-pyrazolo[3,4-b] pyridines

An effective strategy has been developed for the preparation of 3-alkoxymethyl-pyrazolo[3,4-b]pyridines, compounds that are currently not readily accessible by existing synthetic methods. Further manipulation of these compounds allows for access to 3-alkoxymethyl-pyrazolo[3,4-b]pyridines with a variety of substitution patterns as well as 3-aminomethyl-pyrazolo[3,4-b] pyridines.

Synthesis, crystal structure determination, and biological properties of the DNA-dependent protein kinase (DNA-PK) inhibitor 3-cyano-6-hydrazonomethyl-5-(4-pyridyl)pyrid-[1H]-2-one (OK-1035).

The first reported synthesis of the DNA-PK inhibitor 3-cyano-6-hydrazonomethyl-5-(4-pyridyl)pyrid-[1H]-2-one (OK-1035) is described. The structure of OK-1035 was validated by X-ray crystallography. An IC(50) value of 100 microM was determined for inhibition of DNA-PK, and this is approximately 12-fold higher than that reported previously.