8006-71-1

Upstream product

• 31166-44-6 phenylmethyl 1-piperazinecarboxylate 
• 111-41-1 2-(2-Aminoethylamino)ethanol 
• 110-85-0 piperazine 
• 142-64-3 piperazine dihydrochloride 
• 290-37-9 1,4-pyrazine 
• 75-36-5 acetyl chloride 
• 7647-01-0 hydrogenchloride 
• 67-56-1 methanol 
• 4261-68-1 1-chloro-2-diisopropylaminoethane hydrochloride 
• 7542-23-6 piperazine hydrochloride 
• 5700-04-9 1,3-diazacycloheptane-2-thione 
• 6328-56-9 1,4-bis-(2-chloro-propionyl)-piperazine 
• 5712-71-0 1-(2-hydroxyethyl)piperazine dihydrochloride 
• 75-44-5 phosgene 

Downstream Products

• 197968-56-2 2-[2-(1-piperazinyl)ethoxy]acetamide 
• 179334-14-6 1-[3-(trifluoromethyl)benzoyl]piperazine 
• 873697-75-7 methyl piperazine-1,3-carboxylate hydrochloride 
• 153025-29-7 6-chloro-2-piperazin-1-yl-benzothiazole 
• 863001-13-2 C₁₈H₁₄Cl₂N₄S₂ 
• 42270-37-1 1-thiazol-2-yl-piperazine 
• 131136-87-3 1,4-bis(2-thiazolyl)-1,4-diazacyclohexane 
• 55745-83-0 2-piperazinobenzothiazole 
• 138768-65-7 C₁₈H₁₈N₆ 
• 57260-68-1 2-piperazin-1-yl-1H-benzoimidazole 
• 100861-65-2 1-(3-o-tolyloxy-propyl)-piperazine 
• 139516-64-6 1-(2-fluorobenzoyl)-piperazine 
• 13754-45-5 1-(2-chlorobenzoyl)-piperazine 
• 446845-16-5 C₁₈H₁₆N₄S₂ 

Relevant academic research and scientific papers

Can Heteroarenes/Arenes Be Hydrogenated Over Catalytic Pd/C Under Ambient Conditions?

Hydrogenation of over a dozen aromatic compounds, including both heteroarenes and arenes, over palladium on carbon (Pd/C, 1–100 molpercent) with H2-balloon pressure at room temperature is reported. Analyses using pyridine as a model substrate revealed that acetic acid was the best solvent, as using only 1 molpercent Pd/C provided piperidine quantitatively. Substrate scope analysis and density functional theory calculations indicated that reaction rates are highly dependent on frontier molecular orbital characteristics and the steric bulkiness of substituents. Moreover, the established method was used for the concise synthesis of the anti-Alzheimer drug donepezil (Aricept?).

Synthesis method of cinnamyl piperazine

The invention discloses a synthesis method of cinnamyl piperazine. The method includes the steps of: a) adding a solvent into a reaction kettle and adding piperazine to uniformly dissolve the piperazine, dropwisely adding hydrochloric acid at 20-25 DEG C until the pH of the reaction solution is 2, which is the terminal, and after the reaction is performed for 1 h, cooling the reaction solution to 20 DEG C, and centrifugally spin-filtering the reaction solution to obtain piperazine dihydrochloride; b) adding the solvent into the reaction kettle, adding the piperazine dihydrochloride and the piperazine with stirring at the same time, and performing a reaction at 68-85 DEG C for 0.5-3 h; c) reducing the temperature to 45-55 DEG C, dropwisely adding cinnamyl chloride, and then increasing the temperature to 60-75 DEG C to perform a temperature maintained reaction for 1-4 h, and reducing the temperature to 10-35 DEG C, performing centrifugal separation, sucking a mother liquid into a distillation reaction kettle, heating the distillation mother liquid to recycle the solvent, adding pure water, and dropwisely adding an alkali liquid to regulate the pH to 9-12, and adding chloroform to perform extraction, drying the mixture, and evaporate-drying the chloroform to obtain the cinnamyl piperazine. The synthesis method reduces production steps and pollutant emission, and is more suitable for modern industrial production.

A N, 6 diphenyl pyrimidine -4 - amine Bcr - Abl inhibitor and its preparation method and application (by machine translation)

The invention discloses a N, 6 diphenyl pyrimidine - 4 - amine Bcr - Abl inhibitor and its preparation method and application, the structural formula of the inhibitor for the wherein R is a single substituent or double-substituent, substituent is alkyl or halogen; R1 As a single substituent or double-substituent, substituent is alkyl or halogen. The series of inhibitors in vitro ABL1 kinase restraining effects, and can inhibit the proliferation of tumor cells, can be used for anti-tumor pharmaceutical preparation, in particular CML (chronic granulocytic leukemia) drug. The invention provides N, 6 diphenyl pyrimidine - 4 - amine Bcr - Abl inhibitor preparation method, raw materials are apt, mild reaction conditions, the reaction process is simple in operation, reagent used and cheap. (by machine translation)

A convenient synthesis of 1-aralkyl-4-benzylpiperazine derivatives

An efficient two-step route was developed for the synthesis of 1-aralkyl-4-benzylpiperazine derivatives by a Blanc reaction and alkylation. The key intermediate, N-benzylpiperazine, was prepared in an excellent yield by direct benzylation of commercially available piperazine under metal-free conditions.

A Arylheterocycle chirality bcr - abl inhibitor and its preparation method and application

The invention discloses aromatic heterocyclic biphenyl Bcr-Abl inhibitors as well as a preparation method and application thereof. A structural formula of the inhibitors is shown in the specification, wherein in the structural formula, Ar is aromatic heterocycle; R is a mono-substituent or a di-substituent, and the substituent is alkyl or halogen. The series of inhibitors have a certain inhibiting effect on ABL1 kinase in vitro, can inhibit tumor cell proliferation and can be used for preparing antitumor drugs, especially CML (chronic myelocytic leukemia) drugs. The preparation method of the aromatic heterocyclic biphenyl Bcr-Abl inhibitors, which is provided by the invention, has the advantages of easiness in obtainment of raw materials, mild reaction conditions, simplicity in operation of reaction processes and cheap used reagents.

Iridium-catalyzed condensation of amines and vicinal diols to substituted piperazines

A straightforward procedure is described for the synthesis of piperazines from amines and 1,2-diols. The heterocyclization is catalyzed by [Cp*IrCl2]2 and sodium hydrogen carbonate and can be achieved with either toluene or water as solvent. The transformation does not require any stoichiometric additives and only produces water as the byproduct. The reaction can be performed between a 1,2-diamine and a 1,2-diol or by a double condensation between a primary alkylamine and a 1,2-diol. At least one substituent is required on the piperazine ring to achieve the cyclization in good yield. The mechanism is believed to involve dehydrogenation of the 1,2-diol to the α-hydroxy aldehyde, which condenses with the amine to form the α-hydroxy imine. The latter rearranges to the corresponding α-amino carbonyl compound, which then reacts with another amine followed by reduction of the resulting imine. Piperazines are prepared by [Cp*IrCl 2]2-catalyzed heterocyclization of 1,2-diols with either 1,2-diamines or primary alkylamines. The reaction is performed in toluene or water and requires no stoichiometric additive. The key step in the mechanism is believed to be the isomerization of an α-hydroxy imine to the corresponding α-amino carbonyl compound. Copyright

Substituted 1-propiolylpiperazine compounds, their preparation and use

Substituted 1-propiolylpiperazine compounds corresponding to formula I in which X denotes N or C—R2, and n is an integer from 0 to 8, a method for producing such substituted 1-propiolylpiperazine compounds, pharmaceutical compositions containing such substituted 1-propiolylpiperazine compounds, and the use of such substituted 1-propiolylpiperazine compounds for modulating mGluR5 receptor activity or for treating or inhibiting pain and various other conditions, especially conditions at least partly mediated by the mGluR5 receptor.

Optimisation of conditions for O-benzyl and N-benzyloxycarbonyl protecting group removal using an automated flow hydrogenator

A versatile, fully automated flow hydrogenator has been developed that is able to perform sequential flow optimisation experiments, flow library hydrogenation, or iterative scale-up hydrogenation. The behaviour of a palladium catalyst in effecting removal of O-benzyl and N-benzyloxycarbonyl protecting groups has been investigated. Significant observations relating to maintaining optimal throughput are reported. A small library of peptidic derivatives has been deprotected in high yield and purity.

PROCESS FOR PRODUCING PIPERAZINE DERIVATIVE

A process for producing a compound represented by the following general formula or its salt: (1) wherein A represents a lower alkylene group; characterized by comprising reacting a single salt of piperazine represented by the following formula: (2) wherein XH represents a salt-forming organic acid or inorganic acid; with a compound represented by the following general formula: (3) wherein A has the same meaning as defined above; and Y represents an acid residue.

Preparation of N1-(2'-pyridyl)-1,2-propanediamine sulfamic acid and its use in the synthesis of biologically active piperazines

A process for making an N1-(2′-pyridyl)-1,2-alkanediamine sulfamic acid of formula II by reacting a compound of formula I with NH2R′ wherein R and R′ are as defined in the specification. The invention also includes the compound of formula II, and optical isomers thereof. The compound of formula II is an intermediate useful for making chiral piperazine derivatives which are active at the 5-HT1A receptor.