1615254-09-5

Basic information

• Product Name: (S)-tert-butyl (1-(5-fluoro-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)carbamate
• Synonyms: (S)-tert-butyl (1-(5-fluoro-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)carbamate
• CAS NO: 1615254-09-5
• Molecular Weight: 383.422
• Mol File: 1615254-09-5.mol
• Article Data: 4

Chemical Properties

• CAS DataBase Reference: (S)-tert-butyl (1-(5-fluoro-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)carbamate(CAS DataBase Reference)
• NIST Chemistry Reference: (S)-tert-butyl (1-(5-fluoro-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)carbamate(1615254-09-5)
• EPA Substance Registry System: (S)-tert-butyl (1-(5-fluoro-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)carbamate(1615254-09-5)

Safety Data

• Hazardous Substances Data: 1615254-09-5(Hazardous Substances Data)

Upstream product

• 15761-38-3 L-N-Boc-Ala 
• 434-76-4 2-amino-6-fluorobenzoic acid 
• 62-53-3 aniline 
• 1417456-04-2 2-amino-6-fluoro-N-phenyl-benzamide 
• 870281-83-7 2-fluoro-6-nitro-N-phenyl-benzamide 
• 385-02-4 6-fluoro-2-nitrobenzoic acid 

Downstream Products

• 1615255-70-3 (S)-2-(1-aminoethyl)-5-fluoro-3-phenylquinazolin-4(3H)-one 
• 1146702-54-6 (S)-2-(1-((7H-Purin-6-yl)amino)ethyl)-5-fluoro-3-phenylquinazolin-4(3H)-one 

Relevant articles and documents

Synthesis and biological evaluation of novel purinyl quinazolinone derivatives as PI3Kδ-specific inhibitors for the treatment of hematologic malignancies

Phosphatidylinositol 3-kinases (PI3Ks) mediate intracellular signal transduction. Aberrant PI3K signaling is associated with oncogenesis and disease progression in solid tumors and hematologic malignancies. Idelalisib (1), a first-in-class PI3Kδ inhibitor for the treatment of hematologic malignancies, was developed, but its sales were limited by black box warnings due to unexpected adverse effects. Therefore, to overcome these adverse events, various quinazolinone derivatives were synthesized and evaluated in vitro based on their inhibitory activity against the PI3K enzyme and the viability of cell lines such as MOLT and SUDHL. Among them, 6f (IC50 = 0.39 nM) and 6m (IC50 = 0.09 nM) showed excellent enzyme activity, and 6m displayed an approximately four-fold higher selectivity for PI3Kγ/δ compared with Idelalisib (1). Furthermore, in vivo PK experiments with 6f and 6m revealed that 6f (AUClast = 81.04 h*ng/mL, Cmax = 18.34 ng/mL, Tmax = 0.5 h, t1/2 = 10.2 h in 1 mpk dose) had improved PK compared with 1. Finally, further experiments will be conducted with 6f selected as a candidate, and the potential for it to be developed as a treatment with good efficacy for hematologic malignancies will be determined.

Substituted aminopyrimidine compounds and their method and use thereof

The invention relates to a new aminopyrimidine compound and an application thereof as a drug for treating disorder or diseases related to PI3-kinase abnormity in a free form or a pharmaceutically acceptable salt and preparation form. The invention also relates to a pharmaceutical composition which contains the new aminopyrimidine compound and an application of the pharmaceutical composition in treating mammal disorder or diseases and especially treating human disorder or diseases related to the PI3-kinase abnormity, such as treatment of immunity and inflammatory diseases of PI3-kinase regulation which plays a leading role in a leucocyte function and treatment of proliferative diseases which are related to PI3-kinase activity and include but not limited to leukaemia and solid tumor.