1314138-13-0

Basic information

• Product Name: 5,6-dihydro-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-4H-Pyrrolo[1,2-b]pyrazole
• Synonyms: 5,6-dihydro-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-4H-Pyrrolo[1,2-b]pyrazole;3-(tetramethyl-1,3,2-dioxaborolan-2-yl)-4H,5H,6H-pyrrolo[1,2-b]pyrazole;3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole
• CAS NO: 1314138-13-0
• Molecular Formula: C₁₂H₁₉BN₂O₂
• Molecular Weight: 234.10246
• Mol File: 1314138-13-0.mol
• Article Data: 5

Chemical Properties

• Boiling Point: 361.1±30.0 °C(Predicted)
• Appearance: /
• Density: 1.16±0.1 g/cm3(Predicted)
• PKA: 2.59±0.20(Predicted)
• CAS DataBase Reference: 5,6-dihydro-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-4H-Pyrrolo[1,2-b]pyrazole(CAS DataBase Reference)
• NIST Chemistry Reference: 5,6-dihydro-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-4H-Pyrrolo[1,2-b]pyrazole(1314138-13-0)
• EPA Substance Registry System: 5,6-dihydro-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-4H-Pyrrolo[1,2-b]pyrazole(1314138-13-0)

Safety Data

• Hazardous Substances Data: 1314138-13-0(Hazardous Substances Data)

Usage

Uses

3-(Tetramethyl-1,3,2-dioxaborolan-2-yl)-4H,5H,6H-pyrrolo[1,2-b]pyrazole (cas# 1314138-13-0) is a useful reagent for preparation of pyrimidine derivatives for use as human PI3K-delta inhibitors.

Upstream product

• 796729-10-7 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole-3-carboxylic acid 
• 61676-62-8 2-Isopropoxy-4,4,5,5-tetramethyl-1,3,2-dioxaborolane 
• 76-09-5 2,3-dimethyl-2,3-butane diol 
• 174790-35-3 3-bromo-5,6-dihydro-4H-pyrrolo<1,2-b>pyrazole 
• 5419-55-6 Triisopropyl borate 
• 107862-65-7 5,6-dihydro-4H-pyrrolo<1,2-b>pyrazole 
• 174790-34-2 3-(3-chloropropyl)-1H-pyrazole 
• 1429913-29-0 1,2-dibromo-6-chlorohexan-3-one 
• 76328-94-4 6-chlorohexa-1-en-3-one 

Relevant articles and documents

Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies

A CDK9 inhibitor having short target engagement would enable a reduction of Mcl-1 activity, resulting in apoptosis in cancer cells dependent on Mcl-1 for survival. We report the optimization of a series of amidopyridines (from compound 2), focusing on properties suitable for achieving short target engagement after intravenous administration. By increasing potency and human metabolic clearance, we identified compound 24, a potent and selective CDK9 inhibitor with suitable predicted human pharmacokinetic properties to deliver transient inhibition of CDK9. Furthermore, the solubility of 24 was considered adequate to allow i.v. formulation at the anticipated effective dose. Short-term treatment with compound 24 led to a rapid dose- and time-dependent decrease of pSer2-RNAP2 and Mcl-1, resulting in cell apoptosis in multiple hematological cancer cell lines. Intermittent dosing of compound 24 demonstrated efficacy in xenograft models derived from multiple hematological tumors. Compound 24 is currently in clinical trials for the treatment of hematological malignancies.

ARYLOXYMETHYL CYCLOPROPANE DERIVATIVES AS PDE10 INHIBITORS

The present invention is directed to aryloxymethyl cyclopropane derivatives which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

2-PYRIDYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (SYK) INHIBITORS

The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.