91910-75-7

Upstream product

• 95-92-1 oxalic acid diethyl ester 
• 103-79-7 1-phenyl-acetone 
• 103-82-2 phenylacetic acid 
• 95092-10-7 N-methoxy-N-methyl-2-phenylacetamide 
• 698-87-3 3-phenyl-2-propanol 

Downstream Products

• 99846-32-9 2,4-dioxo-5-phenyl-valeric acid 
• 595610-42-7 ethyl 3-benzyl-1H-pyrazole-5-carboxylate 
• 1384129-90-1 C₂₇H₂₆FNO₄ 
• 1384167-75-2 C₂₆H₂₃FN₂O₂ 
• 1384167-65-0 C₂₄H₁₉FN₂O₂ 
• 1399859-23-4 2-(hydroxymethyl)-4-phenylpenta-1,4-dien-3-one 

Relevant academic research and scientific papers

ORGANIC ARSENIC-BASED TYPE II PYRUVATE KINASE INHIBITOR AS WELL AS PREPARATION METHOD THEREFOR AND USE THEREOF

Provided by the present invention are an organic arsenic-based type II pyruvate kinase inhibitor as well as a preparation method therefor and a use thereof. Specifically, a PKM2 inhibitor of the present invention is a compound represented by formula I, or a pharmaceutically acceptable salt thereof, or a stereoisomer or tautomer, a hydrate or a solvate thereof, wherein, X1, X2, R1, R2, R3, R4, R5 and n are as defined in the description. The compound of the present invention has a high inhibitory activity and high specificity for PKM2 and is well suited for the preparation of a drug inhibiting tumors by inhibiting a PKM2 pathway.

Ru-Catalyzed Chemo- and Enantioselective Hydrogenation of β-Diketones Assisted by the Neighboring Heteroatoms

A highly chemo- and enantioselective hydrogenation of β-diketones was achieved by using [Ru(benzene)(S)-SunPhosCl]Cl for consistency in THF. The neighboring heteroatoms played important roles in guaranteeing the reactivity and controlling the chemoselectivity. These results suggested a potential approach for the clean and facile synthesis of functionalized chiral β-hydroxy ketones, which could otherwise be prepared through much less step-economic transformations.

HETEROCYCLIC INHIBITORS OF MCT4

Disclosed herein are compounds and compositions useful in the treatment of MCT4 mediated diseases, such as proliferative and inflammatory diseases, having the structure of Formula I: Methods of inhibition MCT4 activity in a human or animal subject are also provided.

PYRROLIDINE AMIDE COMPOUNDS AS HISTONE DEMETHYLASE INHIBITORS

The present invention relates to compounds of formula (I) useful as inhibitors of one or more histone demethylses, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and the compounds for use in methods for the treatment of various disorders. Formula (I): or a salt thereof, wherein: A is selected from the group consisting of:

Concise synthesis of α-(hydroxymethyl) alkyl and aryl vinyl ketones

2,4-Diketoesters 2 have first been reported as starting materials for the synthesis of a new class of α-hydroxymethyl-α,β-unsaturated ketones 3. Thus, under heterogeneous liquid-liquid medium in the presence of concentrated aqueous potassium carbonate as a base, both aliphatic and aromatic 2,4-dioxoalkanoates 2 react with aqueous formaldehyde to afford the corresponding ketones 3 in fair to good yields. Copyright Taylor & Francis Group, LLC.

Discovery of pyrazole carboxylic acids as potent inhibitors of rat long chain l-2-hydroxy acid oxidase

Long chain l-2-hydroxy acid oxidase 2 (Hao2) is a peroxisomal enzyme expressed in the kidney and the liver. Hao2 was identified as a candidate gene for blood pressure (BP) quantitative trait locus (QTL) but the identity of its physiological substrate and its role in vivo remains largely unknown. To define a pharmacological role of this gene product, we report the development of selective inhibitors of Hao2. We identified pyrazole carboxylic acid hits 1 and 2 from screening of a compound library. Lead optimization of these hits led to the discovery of 15-XV and 15-XXXII as potent and selective inhibitors of rat Hao2. This report details the structure activity relationship of the pyrazole carboxylic acids as specific inhibitors of Hao2.

Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor

A series of 3-aryl-5-acylpiperazinyl-pyrazoles (e.g., 3a-b) initially identified through a high-throughput screening campaign using the aequorin Ca2+ bioluminescence assay as novel, potent small molecule antagonists of the G protein-coupled hum

PYRAZOLE DERIVATIVES AS S1P1 AGONISTS

The present invention relates to a compound of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by sphingosine-1-phosphate receptors (S1P1) agonists.

New pyrazole derivatives

The present invention relates to a compound of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by sphingosine-1-phosphate receptors (S1P1) agonists.

Agonist lead identification for the high affinity niacin receptor GPR109a

A strategy for lead identification of new agonists of GPR109a, starting from known compounds shown to activate the receptor, is described. Early compound triage led to the formulation of a binding hypothesis and eventually to our focus on a series of pyrazole acid derivatives. Further elaboration of these compounds provided a series of 5,5-fused pyrazoles to be used as lead compounds for further optimization.