14547-83-2

Upstream product

• 138023-09-3 N-(4-bromobenzylidene)pyridin-2-amine 
• 504-29-0 2-aminopyridine 
• 1122-91-4 4-bromo-benzaldehyde 
• 14150-95-9 2-aminopyridine N-oxide 
• 586-76-5 4-Bromobenzoic acid 
• 5195-29-9 4-bromophenylglyoxal 
• 1422715-22-7 2-(4-bromophenyl)-N-(pyridin-2-yl)imidazo[1,2-a]pyridin-3-amine 
• 99-90-1 para-bromoacetophenone 
• 80352-42-7 1-(4-bromophenyl)-2,2-dihydroxyethanone 
• 34658-66-7 2-(4-bromophenyl)imidazo[1,2-a]pyridine 
• 1878-68-8 2-(4-bromophenyl)-acetic acid 
• 586-75-4 4-chlorobenzoyl chloride 
• 10342-83-3 4'-Bromopropiophenone 
• 4981-64-0 1-(4-bromophenyl)-1-butanone 

Downstream Products

• 1427204-28-1 4-bromo-N-(dimethylcarbamoyl)-N-(pyridin-2-yl)benzamide 
• 1427204-34-9 4-bromo-N-(diethylcarbamoyl)-N-(pyridin-2-yl)benzamide 
• 850568-25-1 4-(pyridin-2-yl-aminocarbonyl)benzeneboronic acid 
• 1420478-89-2 (S)-2-((1-(4-(pyridin-2-ylcarbamoyl)phenyl)-8-amino)imidazole[1,5-a]pyrazin-2-yl)pyrrolidine1-yl-carboxylic acid benzyl ester 

Relevant academic research and scientific papers

A dual chemosensor for Cu2+and Fe3+based on π-extend tetrathiafulvalene derivative

A new dual chemosensor (TTF-PBA) for Fe3+and Cu2+in different signal pathways was designed and synthesized. The absorption spectrum, fluorescence spectrum and cyclic voltammograms changed in the presence of Cu2+and Fe3+. The optical color changed within 5?s from yellow to orange upon the addition of Cu2+, and it changed to dark yellow when Fe3+existed. The cyclic voltammogram of Cu2+/TTF-PBA changed from Eox?=?0.50?V, Ered?=?0.32?V to Eox?=?0.64?V, Ered?=?0.80?V (vs Ag/AgCl) upon the addition of 2.0 equiv. Cu2+. As for Fe3+/TTF-PBA, its oxidation wave disappeared, and its reduction wave appeared at Ered?=??0.59?V (vs Ag/AgCl) upon the addition of 4.0 equv. Fe3+. The sensor displayed high selectivity for Cu2+and Fe3+over other ions including Pb2+, Zn2+, Ni2+, Ag+, Cr3+, Mn2+, Al3+, Co2+, Pd2+, Hg2+, Fe2+Cd2+, Ce3+, Bi3+and Au3+, the detection limits for Cu2+and Fe3+ion reached as low as 5.33?×?10?7?mol/L and 5.34?×?10?7?mol/L, respectively. Furthermore, when Fe3+existed, Cu2+can be detected sequentially by the sensor through the absorption spectrum and the color change observed by naked-eyes.

NOVEL PROCESS FOR THE PREPARATION OF ACALABRUTINIB AND ITS INTERMEDIATES

The present invention relates to an improved and industrially viable process for the preparation of Acalabrutinib and its Intermediates. The present invention involves less expensive reagents, solvents and the process conditions can be easily adopted for commercial scale. The present invention relates to process for the preparation Acalabrutinib of formula (1) and process for the preparation of Acalabrutinib key starting material.

Co2(CO)8as a Solid CO (g) Source for the Amino Carbonylation of (Hetero)aryl Halides with Highly Deactivated (Hetero)arylamines

Carbonylation of (hetero)aryl iodides/bromides with highly deactivated 2-aminopyridines using Pd-Co(CO)4 bimetallic catalysis is accomplished. The use of Co2(CO)8 as a solid CO(g) source enhanced reaction rates observed when compared to CO(g), and excellent yields highlight the versatility of the developed protocol. A wide range of electronically and sterically demanding heterocyclic amines and (hetero)aryl iodides/bromides employed for this study resulted in excellent yields of amino carbonylated products. The developed methodology was further extended to synthesize Trypanosome brucie and luciferase inhibitors.

Design and synthesis of novel substituted benzyl pyrrolopyrimidine derivatives as selective BTK inhibitors for treating mantle cell lymphoma

Ibrutinib, a potent irreversible Bruton's tyrosine kinase (BTK) inhibitor, was approved by the FDA for treating mantle cell lymphoma (MCL). Although ibrutinib exhibited excellent antitumor activity, it was associated with certain adverse reactions, with o

Copper(I)-catalysed aerobic oxidative selective cleavage of C[sbnd]C bond with DMAP: Facile access to N-substituted benzamides

A base/DMAP system for efficient oxidative cleavage of C(CO)–C(alkyl) bond to generate N-substituted benzamides has been developed in the presence of copper(I) chloride. The usage of inexpensive copper catalyst, broad substrate scope, mild conditions make

Direct Transformation of Alkylarenes into N-(Pyridine-2-yl)amides by C(sp3)–C(sp3) Bond Cleavage

C(sp3)–H bond functionalization and C(sp3)–C(sp3) bond cleavage are very challenging transformations in chemistry. Herein, we report a mild and green methodology for the construction of N-(pyridine-2-yl)amides via tandem C(sp3)–H activation/C–C bond cleavage of alkylarenes. Various N-heterocyclic amides were directly synthesized from alkylarenes in water in moderate to good yields.

Hydroxamic acid derivative containing pyrazolopyrimidine and preparation method and application thereof

The invention provides a hydroxamic acid derivative containing pyrazolopyrimidine and a preparation method and application thereof. The hydroxamic acid derivative containing pyrazolopyrimidine has a structure as shown in a formula I, in the formula I, X is selected from oxygen, acylamino and methylene; Y is selected from methine, substituted methine and nitrogen; Z is selected from methylene, benzyl, piperidyl, pyridyl, pyrrolidinyl, pyrimidinyl, imidazolyl and oxadiazolyl; the piperidyl is shown in the specification, or the carbon end of the piperidyl is connected with the nitrogen end of pyrazole; R is selected from hydrogen, halogen, nitro, amino, substituted amino, cyano, methyl, methoxy and trifluoromethyl; n is any integer from 0 to 7; and when X is oxygen, Y is methine, and Z is R and H, n is not 1. The compound shown in the formula I has BTK and/or HDAC inhibitory activity and has a good growth inhibition effect on lymphoma, especially mantle cell lymphoma.

Aminonorbornane derivative and preparation method and application thereof

The invention discloses an aminonorbornane derivative and a preparation method and application thereof and relates to a compound having a structure represented by a formula I which is described in thespecification or a pharmaceutically acceptable salt, a solvate, an active metabolite, a polymorph, an ester, an optical isomer or a prodrug thereof, a pharmaceutical composition comprising the compound as shown in the formula I, and application of the compound and the pharmaceutical composition as highly selective Bruton's tyrosine kinase (BTK) inhibitors of BTK (C481S) mutants for preparation ofdrugs used for prevention or treatment of heteroimmune diseases, autoimmune diseases or cancer.

1-substituted benzyl pyrazolopyrimidine derivative, preparation method and applications thereof

The invention discloses a 1-substituted benzyl pyrazolopyrimidine derivative, a preparation method and applications thereof, wherein the structure of the 1-substituted benzyl pyrazolopyrimidine derivative is shown as a general formula I, a general formula II or a general formula III, R1 is selected from hydrogen, C1-6 linear chain or branched chain alkyl and trihalomethyl, R2 is selected from hydrogen, halogen, nitro, C1-6 linear chain or branched chain alkyl, trifluoromethyl and cyano, R3 is selected from amino, and R4 is selected from substituted amide group. The compound has a certain BTK inhibition activity.

Method for preparing Acalabrutinib, in particular to method for preparing Acalabrutinib

The invention relates to the field of chemical synthesis, in particular to a chemical synthesis method for preparing Acalabrutinib. The synthesis method of the compound 3 is optimized, wherein the cyano compound 2 is reduced to obtain the compound 3 by adopting a method of generating borane in situ under the conditions of indium trichloride and sodium borohydride. The method is simple and convenient to operate, a special reaction container and hydrogen are not needed for reduction, a high-risk material catalyst nickel is prevented from being adopted, and large-scale production is facilitated.In the preparation of the compound 15, water is used as a solvent, equivalent hydrogen peroxide is added to react the compound 13 with the compound 14 to prepare the compound 15, so that the method iseconomic and environment-friendly, the post-treatment is simple and convenient, and the reaction liquid is directly subjected to centrifugal operation; in addition, the yield is high and can reach 90% or above; and the compound 15 is high in purity and does not need to be further purified, so that the technology can satisfy the requirements of industrial production.