5648-87-3

Upstream product

• 14631-43-7 2-tetrahydrofuran-2-carbonitrile 
• 7677-24-9 trimethylsilyl cyanide 
• 1489-69-6 Cyclopropanecarboxaldehyde 
• 2516-33-8 Cyclopropylmethanol 
• 75-86-5 2-hydroxy-2-methylpropanenitrile 
• 101947-93-7 2-cyclopropyl-2-((trimethylsilyl)oxy)acetonitrile 
• 151-50-8 potassium cyanide 

Downstream Products

• 812652-58-7 3-benzyloxy-5-cyclopropyl-4-imino-oxazolidin-2-one 
• 862461-47-0 3-(4-cyanophenyl)-5-cyclopropyloxazolidin-2,4-dione 
• 752235-30-6 3-benzyloxy-5-cyclopropyl-oxazolidin-2,4-dione 
• 98730-93-9 cyclopropyl-hydroxy-acetic acid methyl ester 
• 1063734-79-1 2-cyclopropylmorpholine 
• 54120-02-4 2-amino-(1RS)-1-cyclopropylethanol 
• 907204-35-7 3-(4-cyanophenyl)-5-cyclopropyl-4-iminooxazolidin-2-one 

Relevant academic research and scientific papers

Nickel-Catalyzed, Reductive C(sp3)?Si Cross-Coupling of α-Cyano Alkyl Electrophiles and Chlorosilanes

A nickel/zinc-catalyzed cross-electrophile coupling of alkyl electrophiles activated by an α-cyano group and chlorosilanes is reported. Elemental zinc is the stoichiometric reductant in this reductive coupling process. By this, a C(sp3)?Si bond can be formed starting from two electrophilic reactants whereas previous methods rely on the combination of carbon nucleophiles and silicon electrophiles or vice versa.

Structure-Based Design of Potent, Selective, and Orally Bioavailable VPS34 Kinase Inhibitors

VPS34 is a class III phosphoinositide 3-kinase involved in endosomal trafficking and autophagosome formation. Inhibitors of VPS34 were believed to have value as anticancer agents, but genetic and pharmacological data suggest that sustained inhibition of V

Access to β-Ketonitriles through Nickel-Catalyzed Carbonylative Coupling of α-Bromonitriles with Alkylzinc Reagents

Herein, we report a nickel-catalyzed carbonylative coupling of α-bromonitriles and alkylzinc reagents with near stoichiometric carbon monoxide to give β-ketonitriles in good yields. The reaction is catalyzed by a readily available and stable nickel(II) pincer complex. The developed protocol tolerates substrates bearing a variety of functional groups, which would be problematic or incompatible with previous synthetic methods. Additionally, we demonstrate the suitability of the method for carbon isotope labeling by the synthesis of 13C-labeled β-ketonitriles and their transformation into isotopically labeled heterocycles.

Stereodivergence in the Ireland-Claisen Rearrangement of α-Alkoxy Esters

A systematic investigation into the Ireland-Claisen rearrangement of α-alkoxy esters is reported. In all cases, the use of KN(SiMe3)2 in toluene gave rearrangement products corresponding to a Z-enolate intermediate with excellent diastereoselectivity, presumably because of chelation control. On the other hand, chelation-controlled enolate formation could be overcome for most substrates through the use of lithium diisopropylamide (LDA) in tetrahydrofuran (THF).

A 4-tert-butoxycarbonyl-2-cyclopropyl morphline preparation method

The invention discloses a 4-tert butoxycarbonyl-2-cyclopropyl morpholine preparation method, cycloprogyl dehyde is used as a starting material for cyaniding, reduction, condensation, cyclization, deoxidization and tert butoxycarbonyl protection to obtain a target product, and the compound is an important pharmaceutical intermediate.

S-IMINO-S-OXO IMINOTHIAZINE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE

In its many embodiments, the present invention provides provides certain S-imino-S-oxo iminothiazine compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein RN, R1A, R1B, R2, R3, R4, ring A, RA, m, L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and may be useful for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.

CGRP RECEPTOR ANTAGONISTS

Compounds of Formula (I): and Formula (II): (where variables R2, R4, A, B, D, W, X, Y and Z are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

O-Protected 3-hydroxy-oxazolidin-2,4-diones: Novel precursors in the synthesis of α-hydroxyhydroxamic acids

O-Protected 3-hydroxyoxazolidin-2,4-diones have been prepared in a novel one-pot reaction by subsequent treatment of cyanohydrins with 1,1′-carbonyldiimidazole and O-protected hydroxylamines followed by acidic hydrolysis of the intermediate 4-imino-oxazolidin-2-ones. Decarbonylation of O-protected 3-hydroxyoxazolidin-2,4-diones by catalytic amounts of sodium methoxide, lithium hydroxide, sodium carbonate and caesium carbonate in methanol afforded O-protected α-hydroxyhydroxamic acids in excellent yields. Their deprotection provided a series of novel α-hydroxyhydroxamic acids.

Benzomorphans useful as NMDA receptor antagonists

Compounds of the formula I STR1 are disclosed. In this formula, R is a member selected from the group consisting of --CR 1 R 2 R 3, hydroxy, an alkoxy group having 1 to 4 carbon atoms and --NR 4 R 5, in which at most one of R 1, R 2 and R 3 is hydrogen and the remainder are each independently selected from the group consisting of an alkyl group having 1 to 4 carbon atoms, an alkenyl group having 2 to 4 carbon atoms, an alkynyl group having 2 to 4 carbon atoms, a cycloalkyl group having 3 to 7 carbon atoms, a cycloalkylalkyl having 4 to 9 carbon atoms and a 3 to 6 membered cyclic ether; R 4 and R 5 are each independently hydrogen or an alkyl group having 1 to 4 carbon atoms; R 6 and R 7 are each independently hydrogen or an alkyl group having 1 to 4 carbon atoms; and R 8 is hydrogen, an alkyl group having 1 to 4 carbon atoms, hydroxy, an alkoxy group having 1 to 4 carbon atoms or halogen. Salts of these compounds are also disclosed. Also disclosed are pharmaceutical compositions of these compounds with a pharmaceutically acceptable carrier, the use of these materials as N-methyl-D-aspartate receptor antagonists, processes for preparing these compounds and salts, and methods to treat cerebral diseases by administering an effective amount of these compounds, salts or compositions.