86477-10-3

Upstream product

• 98262-66-9 3a,4,5,6-tetrahydro-3-oxo-3H-pyrrolo[1,2-c][1,2,3]oxadiazol-7-ium ylide 
• 623-47-2 propynoic acid ethyl ester 
• 86477-05-6 C₅H₆N₂O₂ 

Downstream Products

• 796729-03-8 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole-2-carboxylic acid 
• 796729-10-7 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole-3-carboxylic acid 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors

We report herein the synthesis of novel ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors and the evaluation of pharmaceutical activity against five cancer cell lines (MDA-MB-231, BXPC-3, NCI-H1975, DU145 and 786O). Generally, the majority of compounds displayed strong anti-FAK enzymatic potencies (IC50 1 nM) and could effectively inhibit several class of cancer cell lines within the concentration of 3 μM in comparison with GSK2256098 as a reference. Among them, compound 4o is considered to be the most effective due to high sensitivity in antiproliferation. In culture, 4o could not only inhibit FAK Y397 phosphorylation in MDA-MB-231 cell line, but also trigger apoptosis in a dose-dependent manner. Furthermore, computational docking analysis also suggested that 4o and TAE-226 displayed the similar interaction with FAK kinase domain.

Focal adhesion kinase inhibitor and use

The invention belongs to the field of medicines, relates to a focal adhesion kinase inhibitor and use, in particular relates to a novel focal adhesion kinase inhibitor compound, or stereoisomers, geometric isomers, tautomers, oxynitrides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof, further relates to the use of the compound and pharmaceutical compositions as medicines, in particular the use of the compound and pharmaceutical compositions in manufacture of medicines for treatment or prevention of cancer, pulmonary hypertension, and pathological angiogenesis-related diseases.

PYRAZOLE AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS FOR USE IN THE TREATMENT OF PARKINSON'S DISEASE

Compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3 and A are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease

Selective hydrolysis of ethyl 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole-2- carboxylate and ethyl 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole-3-carboxylate as a key step in the large-scale synthesis of bicyclic heteroaryl carboxyaldehydes

The isomeric mixture of ethyl 5,6-dihydro-4H-pyrrolo[1,2-b]-pyrazole-2- and -3-carboxylates (14 and 15), derived from a proline meso-ionic synthon, demonstrated remarkably different stabilities towards alkaline hydrolysis. On that basis, a non-chromatographic, highly efficient method for their large-scale separation was developed. The desired isomer 14 was converted into 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole-2-carbaldehyde, a key intermediate in the synthesis of bicyclic heteroaryl-substituted 6-alkylidene penems.

Process for synthesizing beta-lactamase inhibitor intermediates

There is provided a process for the preparation of bicyclicheteroaryl carboxaldehydes having the structural Formula I where X and Y are defined in the specification The bicyclic heteroaryl carboxaldehydes are useful as intermediates in the preparation of β-lactamase inhibitors.

A NOVEL PROLIN DERIVED MESO-IONIC SYNTHON

A practical route to the strained 5,6-dihydro-4H-pyrrolopyrazoles has been accomplished by "pyrazolo annulation" on the proline ring, via the novel and strained meso-ionic 5,6-dihydro-4H-pyrrolooxadiazolone (3).