57184-25-5

Usage

Uses

Used in Pharmaceutical Industry:
1-(CYCLOPROPYLMETHYL)PIPERAZINE 97 is used as a key intermediate compound for the synthesis of N-substituted piperazinopyridylsteroid derivatives, specifically abiraterone analogs. These analogs are designed to inhibit the growth and induce pro-apoptosis in human hormone-independent prostate cancer cell lines, making them a promising avenue for the development of novel cancer treatments.
Application Reason:
1-(CYCLOPROPYLMETHYL)PIPERAZINE 97's unique structure allows for the formation of abiraterone analogs, which have shown potential in targeting hormone-independent prostate cancer cells. This makes 1-(CYCLOPROPYLMETHYL)PIPERAZINE 97 a valuable asset in the development of new cancer therapies, particularly for patients with hormone-independent prostate cancer.

InChI:InChI=1/C8H16N2/c1-2-8(1)7-10-5-3-9-4-6-10/h8-9H,1-7H2

Upstream product

• 373608-50-5 4-cyclopropylmethylpiperazine-1-carboxylic acid tert-butyl ester 
• 59878-57-8 1-(cyclopropylcarbonyl)piperazine 

Downstream Products

• 755039-89-5 (trans)-N,N-dibenzyl-4-[4-(cyclopropylmethyl)piperazin-1-yl]cyclohexanamine 
• 755039-88-4 (cis)-N,N-dibenzyl-4-[4-(cyclopropylmethyl)piperazin-1-yl]cyclohexanamine 
• 1186390-26-0 2-(3-(7-(4-(4-(cyclopropylmethyl)piperazine-1-carbonyl)phenyl)quinazolin-4-ylamino)-1H-pyrazol-5-yl)-N-(3-fluorophenyl)acetamide 
• 1229021-70-8 C₂₅H₂₅N₅O 
• 477576-65-1 3-[1-{4-[2-(4-Cyclopropylmethyl-piperazin-1-yl)-2-oxo-ethyl]-3,5-dimethyl-1H-pyrrol-2-yl }-meth-(Z)-ylidene]-5-(2,6-dichloro-phenylmethanesulfonyl)-1,3-dihydro-indol-2-one 
• 548768-88-3 4-Cyclopropylmethyl-piperazine-1-carboxylic acid 4-(2-cyclohexyl-acetylamino)-phenyl ester 
• 548768-82-7 4-Cyclopropylmethyl-piperazine-1-carboxylic acid 4-(4,4-dimethyl-2,6-dioxo-piperidin-1-yl)-phenyl ester 
• 548768-53-2 4-Cyclopropylmethyl-piperazine-1-carboxylic acid 4-[2-(4-chloro-phenyl)-ethylcarbamoyl]-phenyl ester 
• 549510-83-0 4-Cyclopropylmethyl-piperazine-1-carboxylic acid 4-(3-chloro-5-trifluoromethyl-pyridin-2-yloxy)-phenyl ester 

Relevant academic research and scientific papers

Discovery of Novel Apigenin-Piperazine Hybrids as Potent and Selective Poly (ADP-Ribose) Polymerase-1 (PARP-1) Inhibitors for the Treatment of Cancer

Poly (ADP-ribose) polymerase-1 (PARP-1) is a potential target for the discovery of chemosensitizers and anticancer drugs. Amentoflavone (AMF) is reported to be a selective PARP-1 inhibitor. Here, structural modifications and trimming of AMF have led to a series of AMF derivatives (9a-h) and apigenin-piperazine/piperidine hybrids (14a-p, 15a-p, 17a-h, and 19a-f), respectively. Among these compounds, 15l exhibited a potent PARP-1 inhibitory effect (IC50 = 14.7 nM) and possessed high selectivity to PARP-1 over PARP-2 (61.2-fold). Molecular dynamics simulation and the cellular thermal shift assay revealed that 15l directly bound to the PARP-1 structure. In in vitro and in vivo studies, 15l showed a potent chemotherapy sensitizing effect against A549 cells and a selective cytotoxic effect toward SK-OV-3 cells through PARP-1 inhibition. 15l·2HCl also displayed good ADME characteristics, pharmacokinetic parameters, and a desirable safety margin. These findings demonstrated that 15l·2HCl may serve as a lead compound for chemosensitizers and the (BRCA-1)-deficient cancer therapy.

CYCLIN-DEPENDENT KINASE INHIBITING COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS

This invention is in the area of cell cycle inhibiting compounds for the treatment of disorders involving abnormal cellular proliferation, and include selective CDK2 inhibitors for medical therapy and their pharmaceutically acceptable salts and compositions.

Preparation method of Volasertib intermediate 1-cyclopropyl methyl piperazine

The invention provides a preparation method of a Volasertib intermediate 1-cyclopropyl methyl piperazine. The preparation method comprises the following steps: S1, adding N-Boc-piperazine into an inert solvent and triethylamine or pyridine, dropwise adding cyclopropanecarbonyl chloride, adding water for extraction after the reaction ends, obtaining an organic phase, and concentrating the organic phase to remove an organic solvent to obtain a solid; S2, adding the solid obtained in S1 into an ether solvent, then adding sodium borohydride, dropwise adding boron trifluoride-diethyl ether for reaction, quenching the mixture, then extracting the mixture, and concentrating the mixture to remove an organic solvent to obtain a solid; S3, adding the solid obtained in S2 into an alcohol solvent, dropwise adding concentrated hydrochloric acid for reaction, alkalizing the mixture with sodium hydroxide or potassium hydroxide aqueous solution, and performing extraction and concentration in sequenceto obtain the compound 1-cyclopropyl methyl piperazine. The raw materials used in the preparation method are readily available, and the preparation method is low in cost, easy to operate, high in safety, high in product quality and yield, and convenient for large-scale production.

PYRIMIDINE-BASED ANTIPROLIFERATIVE AGENTS

This invention is in the area of pyrimidine-based compounds for the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.

DIHYDROPTERIDINONE DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF

Dihydroperidinone derivatives, preparation process and pharmaceutical use thereof are disclosed. Specially, new dihydroperidinone derivatives represented by general formula (I), wherein each substituent of the general formula (I) is defined as in the description, their preparation process, pharmaceutical compositions comprising said derivatives and their use as therapeutical agents, especially as Plk kinase inhibitors are disclosed.

ACETYLENE DERIVATIVES AS STEAROYL COA DESATURASE INHIBITORS

The present invention provides Stearoyl CoA Desaturase (SCD) inhibitors, hi particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by Stearoyl CoA Desaturase 1 (SCD 1) inhibitors. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by Stearoyl CoA Desaturase (SCD) inhibitors.

NOVEL PHYSIOLGICALLY ACTIVE SUBSTANCES

The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.

1-Alkyl-4-acylpiperazines as a new class of imidazole-free histamine H 3 receptor antagonists

With the aim of identifying structurally novel, centrally acting histamine H3 antagonists, arrays of monoacyldiamines were screened. This led to the discovery of a series of 1-alkyl-4-acylpiperazines which were potent antagonists at the human histamine H3 receptor. The most potent amides had antagonist potencies in the subnanomolar range.