936694-19-8

Usage

Uses

Used in Organic Synthesis:
Tert-Butyl 4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl)piperazine-1-carboxylate is used as a reagent in organic synthesis for the creation of diverse organic compounds. Its unique molecular structure, including the dioxaborolane group, makes it a valuable intermediate in the synthesis of pharmaceuticals, agrochemicals, and other specialty chemicals.
Used in Pharmaceutical Industry:
In the pharmaceutical industry, tert-Butyl 4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl)piperazine-1-carboxylate is utilized as a key building block in the development of new drugs. Its versatility in organic synthesis allows for the creation of molecules with potential therapeutic applications, contributing to the advancement of medicinal chemistry.
Used in Chemical Research:
Tert-Butyl 4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl)piperazine-1-carboxylate is also used in academic and industrial research settings. It serves as a model compound for studying reaction mechanisms and exploring new synthetic methodologies, furthering the understanding of organic chemistry and its applications.

Upstream product

• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 589-15-1 1-bromomethyl-4-bromobenzene 
• 844891-10-7 tert-butyl 4-[(4-bromophenyl)methyl]piperazine-1-carboxylate 
• 73183-34-3 bis(pinacol)diborane 
• 138500-85-3 4-bromomethylphenylboronic acid pinacol ester 

Downstream Products

• 1316807-39-2 tert-butyl 4-(4-(5-nitropyridin-2-yl)benzyl)piperazine-1-carboxylate 
• 1316807-53-0 1-(4-(5-nitropyridin-2-yl)benzyl)piperazine 
• 1316807-70-1 (4-methoxy-phenyl)-[4-(2'-nitro-biphenyl-4-ylmethyl)-piperazin-1-yl]-methanone 
• 1316807-73-4 cyclohexyl(4-((3'-nitrobiphenyl-4-yl)methyl)piperazin-1-yl)methanone 
• 1316807-76-7 1-((3'-nitrobiphenyl-4-yl)methyl)-4-(phenylsulfonyl)piperazine 
• 1316807-79-0 1-(methylsulfonyl)-4-((4'-nitrobiphenyl-4-yl)methyl)piperazine 
• 1316807-82-5 1-{4-[4-(5-nitro-pyridin-2-yl)-benzyl]-piperazin-1-yl}-pentan-1-one 
• 1316807-83-6 {4-[4-(5-nitro-pyridin-2-yl)-benzyl]-piperazin-1-yl}-phenyl-methanone 
• 1316807-88-1 (4-((3'-aminobiphenyl-4-yl)methyl)piperazin-1-yl)(cyclohexyl)methanone 
• 1316808-05-5 (4-((2'-aminobiphenyl-4-yl)methyl)piperazin-1-yl)(4-methoxyphenyl)methanone 
• 1316808-10-2 4'-((4-(phenylsulfonyl)piperazin-1-yl)methyl)biphenyl-3-amine 
• 1316808-13-5 1-(4-(4-(5-aminopyridin-2-yl)benzyl)piperazin-1-yl)pentan-1-one 
• 1316808-16-8 (4-(4-(5-aminopyridin-2-yl)benzyl)piperazin-1-yl)(phenyl)methanone 
• 1316808-29-3 N-(4'-((4-(cyclohexanecarbonyl)piperazin-1-yl)methyl)biphenyl-3-yl)methanesulfonamide 

Relevant academic research and scientific papers

Structure-based design, synthesis, and evaluation of inhibitors with high selectivity for PARP-1 over PARP-2

The poly (ADP-ribose) polymerase (PARP) inhibitors play a crucial role in cancer therapy. However, most approved PARP inhibitors have lower selectivity to PARP-1 than to PARP-2, so they will inevitably have side effects. Based on the different catalytic domains of PARP-1 and PARP-2, we developed a strategy to design and synthesize highly selective PARP-1 inhibitors. Compounds Y17, Y29, Y31 and Y49 showed excellent PARP-1 inhibition, and their IC50 values were 0.61, 0.66, 0.41 and 0.96 nM, respectively. Then, Y49 (PARP-1 IC50 = 0.96 nM, PARP-2 IC50 = 61.90 nM, selectivity PARP-2/PARP-1 = 64.5) was proved to be the most selective inhibitor of PARP-1. Compounds Y29 and Y49 showed stronger inhibitory effect on proliferation in BRCA1 mutant MX-1 cells than in other cancer cells. In the MDA-MB-436 xenotransplantation model, Y49 was well tolerated and showed remarkable single dose activity. The design strategy proposed in this paper is of far-reaching significance for the further construction of the next generation of selective PARP-1 inhibitors.

1,5,7-TRISUBSTITUTED ISOQUINOLINE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF IN MEDICINES

The present disclosure relates to 1,5,7-trisubstituted isoquinoline derivatives, their preparation and pharmaceutical use. In particular, the present disclosure discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof. The definitions of the groups in the formula can be found in the specification and claims.

MERTK DEGRADERS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same.

3-ARYL-5-SUBSTITUTED-ISOQUINOLIN-1-ONE COMPOUNDS AND THEIR THERAPEUTIC USE

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted- 2/-/-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, e

Substituted Hetero-Bicyclic Compounds, Compositions and Medicinal Applications Thereof

The present disclosure provides hetero-bicyclic compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, hydrates, N-oxides, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by Bruton's tyrosine kinase (Btk) activity, The disclosure also relates to the process of preparation of compounds of Formula (I). These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of Bruton's tyrosine kinase (Btk), such as inflammatory and/or autoimmune disorder, cell proliferation, rheumatoid arthritis, psoriasis, psoriatic arthritis, transplant rejection, graft-versus-host disease, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, B-cell malignancies, systemic lupus, erythematosus or other disorders.

SUBSTITUTED HETERO-BICYCLIC COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF

The present disclosure provides hetero-biclyclic compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, hydrates, N-oxides, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by Bruton's tyrosine kinase (Btk) activity, The disclosure also relates to the process of preparation of compounds of Formula (I). These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of Bruton's tyrosine kinase (Btk), such as inflammatory and/or autoimmune disorder, cell proliferation, rheumatoid arthritis, psoriasis, psoriatic arthritis, transplant rejection, graft-versus-host disease, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, B-cell malignancies, systemic lupus, erythematosus or other disorders.

Microwave-mediated synthesis of an arylboronate library

A series of arylboronates has been synthesized from the reaction of 2-(2-, (3-, or (4-(bromomethyl)phenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane 1{1-3} respectively with a range of N-, S-, and O-nucleophiles, using microwave-mediated chemistry. For the synthesis of N- and S-substituted boronates, a supported base, PS-NMM, was employed, and many reactions were complete within 15 min. With O-nucleophiles, a mixture of tetrabutylammonium bromide, potassium carbonate, and sodium hydroxide was employed. The resulting aminomethyl, mercaptomethyl, or alkoxy-/phenoxymethyl-arylboronates were subjected to microwave-mediated Suzuki Miyaura coupling reactions to afford a range of biaryls in moderate to good yields. The X-ray structures of five boronates were determined.

OXAZOLE TYROSINE KINASE INHIBITORS

The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1 : provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.