1017782-93-2

Basic information

• Product Name: tert-butyl 4-(2-formyl-4-nitrophenyl)tetrahydro-1(2H)-pyrazinecarboxylate
• Synonyms: tert-butyl 4-(2-formyl-4-nitrophenyl)tetrahydro-1(2H)-pyrazinecarboxylate
• CAS NO: 1017782-93-2
• Molecular Formula: C₁₆H₂₁N₃O₅
• Molecular Weight: 335.35504
• Mol File: 1017782-93-2.mol
• Article Data: 6

Chemical Properties

• Melting Point: 145-147°
• Appearance: /
• CAS DataBase Reference: tert-butyl 4-(2-formyl-4-nitrophenyl)tetrahydro-1(2H)-pyrazinecarboxylate(CAS DataBase Reference)
• NIST Chemistry Reference: tert-butyl 4-(2-formyl-4-nitrophenyl)tetrahydro-1(2H)-pyrazinecarboxylate(1017782-93-2)
• EPA Substance Registry System: tert-butyl 4-(2-formyl-4-nitrophenyl)tetrahydro-1(2H)-pyrazinecarboxylate(1017782-93-2)

Safety Data

• HazardClass: IRRITANT
• Hazardous Substances Data: 1017782-93-2(Hazardous Substances Data)

Upstream product

• 27996-87-8 2-fluoro-5-nitrobenzaldehye 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 6361-21-3 2-chloro-5-nitrobenzaldehyde 

Downstream Products

• 955369-05-8 4-(2-(hydroxymethyl)-4-nitrophenyl)piperazine-1-carboxylic acid tert-butyl ester 
• 1312603-39-6 4-(2-allyloxymethyl-4-nitrophenyl)piperazine-1-carboxylic acid tert-butyl ester 
• 1312603-45-4 4-(2-allyloxymethyl-4-aminophenyl)piperazine-1-carboxylic acid tert-butyl ester 
• 1312603-54-5 4-{2-allyloxymethyl-4-[4-(3-allyloxymethylphenyl)-pyrimidin-2-ylamino]-phenyl}-piperazine-1-carboxylic acid tert-butyl ester 

Relevant articles and documents

Pyrrolopyrimidine compound, pharmaceutical composition containing thereof, and preparation method and applications

The invention relates to a pyrrolopyrimidine compound represented by formula I, a pharmaceutical composition containing thereof, and a preparation method and applications in preventing or treating Weel protein kinase related diseases.

PYRIMIDOPYRIMIDINONES USEFUL AS WEE-1 KINASE INHIBITORS

The present invention relates to compounds that are useful as inhibitors of the activity of Wee-1 kinase. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in the treatment of cancer and methods of treating cancer.

Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7, 26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27) ,16,21,23-decaene (SB1518), a potent Janus Kinase 2/Fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymphoma

Discovery of the activating mutation V617F in Janus Kinase 2 (JAK2 V617F), a tyrosine kinase critically involved in receptor signaling, recently ignited interest in JAK2 inhibitor therapy as a treatment for myelofibrosis (MF). Herein, we describe the design and synthesis of a series of small molecule 4-aryl-2-aminopyrimidine macrocycles and their biological evaluation against the JAK family of kinase enzymes and FLT3. The most promising leads were assessed for their in vitro ADME properties culminating in the discovery of 21c, a potent JAK2 (IC50 = 23 and 19 nM for JAK2 WT and JAK2V617F, respectively) and FLT3 (IC50 = 22 nM) inhibitor with selectivity against JAK1 and JAK3 (IC50 = 1280 and 520 nM, respectively). Further profiling of 21c in preclinical species and mouse xenograft and allograft models is described. Compound 21c (SB1518) was selected as a development candidate and progressed into clinical trials where it is currently in phase 2 for MF and lymphoma.