256951-79-8

Basic information

• Product Name: Tert-Butyl 4-Cyano-4-(4-Fluorophenyl)Piperidine-1-Carboxylate
• Synonyms: Tert-Butyl 4-Cyano-4-(4-Fluorophenyl)Piperidine-1-Carboxylate;1-Boc-4-cyano-4-(4-fluorophenyl)-piperidine
• CAS NO: 256951-79-8
• Molecular Formula: C₁₇H₂₁FN₂O₂
• Molecular Weight: 304.36
• Mol File: 256951-79-8.mol

Chemical Properties

• Appearance: /
• CAS DataBase Reference: Tert-Butyl 4-Cyano-4-(4-Fluorophenyl)Piperidine-1-Carboxylate(CAS DataBase Reference)
• NIST Chemistry Reference: Tert-Butyl 4-Cyano-4-(4-Fluorophenyl)Piperidine-1-Carboxylate(256951-79-8)
• EPA Substance Registry System: Tert-Butyl 4-Cyano-4-(4-Fluorophenyl)Piperidine-1-Carboxylate(256951-79-8)

Safety Data

• Hazardous Substances Data: 256951-79-8(Hazardous Substances Data)

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 258500-80-0 4-(4-fluorophenyl)-1-methylpiperidine-4-carbonitrile 
• 459-22-3 4-fluorophenylacetonitrile 
• 55-86-7 mechlorethamine hydrochloride 

Downstream Products

• 669068-96-6 1-acetyl-4-(4-fluorophenyl)piperidine-4-carbonitrile 

Relevant articles and documents

Design, synthesis and biological evaluation of AKT inhibitors bearing a piperidin-4-yl appendant

A series of AKT inhibitors possessing a piperidin-4-yl side chain was designed and synthesized. Some of them showed high AKT1 inhibitory activity and potent anti-proliferative effect on PC-3 prostate cancer cells in the preliminary screening. Further studies revealed the most potent compound, 10h, as a pan-AKT inhibitor. Compound 10h was able to inhibit the cellular phosphorylation of AKT effectively and induce apoptosis of PC-3 cells. It also showed high metabolic stability in human liver microsomes. Preclinical characterization of 10h, a promising lead AKT inhibitor, as a potential anti-prostate cancer therapeutic needs to be further investigated.

PIPERIDINE OR PIPERAZINE LINKED IMIDAZOLE AND TRIAZOLE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG

The present invention relates to piperidine or piperazine linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhbiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.

PIPERIDINE OR PIPERAZINE LINKED IMIDAZOLE AND TRIAZOLE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG

The piperidine or piperazine linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug are provided. The compounds of the invention are useful in human and veterinary medicine for inhibiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.

Preparation of 2,3-dihydro-1H-spiro[isoquinoline-4,4′-piperidine] via an N-sulfonyl Pictet-Spengler reaction

A high yielding synthesis of variously substituted 2,3-dihydro-1H-spiro[isoquinoline-4,4′-piperidine] is reported. N-(2-nitrophenyl)sulfonyl was successfully used as both an activating and protecting group for the key Pictet-Spengler reaction.

Alpha 1A adrenergic receptor antagonists

This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

Dihydropyridinones and pyrrolinones useful as alpha 1A adrenoceptor antagonists

Novel dihydropyridinone and pyrrolinone compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha1aadrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha1areceptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.