68535-55-7

Upstream product

• 54781-19-0 2-(trimethylsiloxy)cyclohexa-1,3-diene 
• 37972-24-0 2-ethynylpyrimidine 
• 71597-85-8 (p-hydroxyphenyl)boronic acid 
• 4595-60-2 2-bromopyrimidine 
• 5720-07-0 4-methoxyphenylboronic acid 
• 1722-12-9 2-chloropyrimidine 
• 69491-44-7 2-(4-methoxy-phenyl)-pyrimidine 

Downstream Products

• 925437-86-1 2-(4-{3-[4-(1-trityl-1H-imidazol-4-ylmethyl)-piperidin-1-yl]-propoxy}-phenyl)-pyrimidine 

Relevant academic research and scientific papers

FLUOROALLYLAMINE DERIVATIVE AND USE THEREOF

The present invention relates to a fluoroallylamine derivative and use thereof. In particular, the present invention relates to a compound as shown in Formula I, a prodrug, an isomer, an isotope-labeled compound, a solvate or a pharmaceutically acceptable salt thereof, which has VAP-1/SSAO inhibitory activity, and can be used for treating a disease associated with VAP-1/SSAO overactivity.

VASCULAR ADHESION PROTEIN-1 (VAP-1) MODULATORS AND THERAPEUTIC USES THEREOF

Disclosed herein are small molecule Vascular Adhesion Protein- 1 (VAP-1) modulator compositions, pharmaceutical compositions, the use and preparation thereof.

SSAO INHIBITOR

The present invention provides an SSAO inhibitor and an application thereof in preparing a drug for treating a disease related to SSAO. In particular, the present invention provides a compound shown in formula (IV) and a pharmaceutically acceptable salt thereof.

NOVEL NUCLEOSIDE PHOSPHORAMIDATE COMPOUND AND USE THEREOF

The present invention provides a novel nucleoside phosphoramidate compound, or a stereoisomer, salt, hydrate, solvate or crystal thereof for the treatment of Flaviviridae family viral infection, especially hepatitis C viral infection. The present invention also provides the pharmaceutical composition comprising a compound of the present invention, or a stereoisomer, salt, hydrate, solvate or crystal thereof and a use of the compound or the composition of the present invention in the treatment of Flaviviridae family viral infection, especially hepatitis C viral infection. The compound of the present invention has a good anti-HCV effect.

Synthesis of functionalized arylpyridines and -pyrimidines by domino [4+2]/retro [4+2] cycloadditions of electron-rich dienes with alkynylpyridines and -pyrimidines

Aryl-substituted pyridines and pyrimidines were prepared by [4+2] cycloadditions of alkynyl-substituted pyridines and -pyrimidines with electron-rich dienes. The reactions proceed by formation of a bridged cycloadduct and subsequent thermal extrusion of ethylene. The pyridine moiety plays a crucial role for the success of the reaction.

Palladium-Catalyzed Regioselective C-H Bond ortho-Acetoxylation of Arylpyrimidines

An efficient and regioselective palladium-catalyzed ortho C-H acetoxylation reaction was developed to afford, ortho monoacetoxylated arylpyrimidmes in good to excellent yields by using cupric trifluoroacetate as a cocatalyst. A wide variety of oxygenated

Palladium-catalyzed monoselective halogenation of C-H bonds: Efficient access to halogenated arylpyrimidines using calcium halides

A wide variety of ortho-halogenated arylpyrimidines were prepared with high monoselectivity and functional-group tolerance by using calcium halides as crucial halogenating agents and cupric trifluoroacetate as oxidant in the presence of air.

HETEROCYCLIC COMPOUNDS AND METHODS OF USE

In one aspect, the present invention provides for a compound of Formula I; in which the variable X1a, X1b, X1c, X1d, Q, A, R1, B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.

Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl)methyl] piperidine series of histamine H3 receptor antagonists

A novel series of histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine template displaying low CYP2D6 and CYP3A4 inhibitory profiles has been identified. Structural features responsible for the reduction of P450 activity, a typical liability of 4-substituted imidazoles, have been established.

Synthesis and analgesic-antiinflammatory activity of some 4- and 5-substituted heteroarylsalicylic acids

We have made a series of 4- and 5-aryl- and 4- and 5-heteroarylsalicylic acid derivatives with the objective of reducing gastric irritation and increasing potency. Here we describe a series of 4- and 5-heterocyclic salicylic acids and their antiinflammatory-analgesic potencies measured in comparison to aspirin. An improvement of the therapeutic index over aspirin of 100 was achieved; however, the heterocyclic salicylic acids lacked antipyretic activity. Some physicochemical parameters which may bear on the antiinflammatory activity of these compounds are discussed.