Category: 136624-42-5

Recommanded Product: 136624-42-5On June 13, 2016, Stotani, Silvia; Lorenz, Christoph; Winkler, Matthias; Medda, Federico; Picazo, Edwige; Ortega Martinez, Raquel; Karawajczyk, Anna; Sanchez-Quesada, Jorge; Giordanetto, Fabrizio published an article in ACS Combinatorial Science. The article was 《Design and Synthesis of Fsp3-Rich, Bis-Spirocyclic-Based Compound Libraries for Biological Screening》. The article mentions the following:

The exploration of innovative chem. space is a critical step in the early phases of drug discovery. Bis-spirocyclic frameworks occur in natural products and other biol. relevant metabolites and show attractive features, such as mol. compactness, structural complexity, and three-dimensional character. A concise approach to the synthesis of bis-spirocyclic-based compound libraries starting from readily available com. reagents and robust chem. transformations has been developed. A number of novel bis-spirocyclic scaffold examples, as implemented in the European Lead Factory project, is presented. The experimental process involved the reaction of 4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5Recommanded Product: 136624-42-5)

4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5) belongs to anime. Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic amines have the nitrogen atom connected to an aromatic ring.Important amines include amino acids, biogenic amines, trimethylamine, and aniline. Inorganic derivatives of ammonia are also called amines, such as monochloramine (NClH2).Recommanded Product: 136624-42-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

The author of 《4-Substituted piperidines. III. Reduction of 1-benzyl-4-cyano-4-tert-aminopiperidines with lithium aluminum hydride》 were Hermans, Bert; van Daele, Paul; van de Westeringh, Cornelis; van der Eycken, Cyriel; Boey, Jozef; Janssen, Paul A. J.. And the article was published in Journal of Medicinal Chemistry in 1966. Safety of 4-Amino-1-benzylpiperidine-4-carbonitrile The author mentioned the following in the article:

cf. CA 63, 16298f. The reduction of 1-benzyl-4-cyano-4-tert-aminopiperidines with LiAlH4 is described; this reduction results in dentrilation, whereas the same reduction of the corresponding primary carboxamides yields the expected primary amines, which can easily be acylated. The obtained compounds are debenzylated, after which other substituents are introduced. These new compounds are virtually devoid of hypotensive or central nervous system depressant activity. In the part of experimental materials, we found many familiar compounds, such as 4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5Safety of 4-Amino-1-benzylpiperidine-4-carbonitrile)

4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5) belongs to anime. Reaction with nitrous acid (HNO2), which functions as an acylating agent that is a source of the nitrosyl group (―NO), converts aliphatic primary amines to nitrogen and mixtures of alkenes and alcohols corresponding to the alkyl group in a complex process. This reaction has been used for analytical determination of primary amino groups in a procedure known as the Van Slyke method.Safety of 4-Amino-1-benzylpiperidine-4-carbonitrile

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Samnick, Samuel; Brandau, Wolfgang; Sciuk, Joachim; Steinstraesser, Axel; Schober, Otmar published an article in Nuclear Medicine and Biology. The title of the article was 《Synthesis, characterization and biodistribution of neutral and lipid-soluble 99mTc-bisaminoethanethiol spiperone derivatives: possible ligands for receptor imaging with SPECT》.Formula: C13H17N3 The author mentioned the following in the article:

Using parts of the mol. structure of spiperone, two new ligand systems for complexation with 99mTc were prepared to develop potential receptor imaging agents for SPECT. The bis-aminoethanethiols (BAT): 1-benzyl-4-(2-mercapto-2-methyl-4-aza-pentyl)-4-(2-mercapto-2-methyl-propylamino)-piperidine (benzylpiperidyl-BAT, BP-BAT) and 1-[3-(4-fluorobenzoyl)-propyl]-4-(2-mercapto-2-methyl-4-aza-pentyl)-4-(2-mercapto-2-methyl-propylamino)-piperidine (butyrophenoylpiperidyl-BAT, BUP-BAT) form stable, neutral and lipid soluble complexes with 99mTc at pH ≥11 using SnCl2 as reducing agent in nearly quant. radiochem. yields. The biodistribution of 99mTc-BP-BAT and 99mTc-BUP-BAT in rats showed a moderate clearance from blood and low uptake and retention in the liver, whereas brain showed moderate uptake with prolonged retention. On the other hand, significant accumulations and retentions were observed in heart, kidney and lung with increasing oxygen/blood ratios up to 24 h. Within 24 h p.i. 22 and 29% of the injected dose (i.d.) of 99mTc-BP-BAT and 99mTc-BUP-BAT were eliminated by hepatobiliary excretion whereas 22% i.d. of both 99mTc-BAT complexes were excreted into the urine. Although first biodistribution studies of 99mTc-BP-BAT and 99mTc-BUP-BAT in rats showed relatively low brain uptake, the high uptake in peripheral, receptor rich organs indicates that compounds of this type may be used as a basis for further structural modification to develop agents with optimal properties for cerebral or peripheral receptor imaging with SPECT. In the experiment, the researchers used many compounds, for example, 4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5Formula: C13H17N3)

4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5) belongs to anime. Amine, any member of a family of nitrogen-containing organic compounds that is derived, either in principle or in practice, from ammonia (NH3). Naturally occurring amines include the alkaloids, which are present in certain plants; the catecholamine neurotransmitters (i.e., dopamine, epinephrine, and norepinephrine); and a local chemical mediator, histamine, that occurs in most animal tissues.Formula: C13H17N3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 1965,Journal of Medicinal Chemistry included an article by Hermans, Bert; Daele, Paul van; Westeringh, Cornelis van de; Eycken, Cyriel van der; Boey, Jozef; Janssen, Paul A. J.. Application In Synthesis of 4-Amino-1-benzylpiperidine-4-carbonitrile. The article was titled 《4-Substituted piperidines. II. Reaction of 1-benzyl-4-cyano-4-tertiaryaminopiperidines with organometallic compounds》. The information in the text is summarized as follows:

cf. CA 61, 10652f. The reaction of 1-benzyl-4-cyano-4-tertiary-aminopiperidines with organomagnesium and organolithium compounds is described. Reaction of these α-amino nitriles with Grignard reagents results in replacement of the nitrile group, whereas with the organolithium compounds normal ketone formation takes place. The resulting products are debenzylated, whereafter other substituents are introduced. Some of the obtained products show central nervous system depressant activity. In the part of experimental materials, we found many familiar compounds, such as 4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5Application In Synthesis of 4-Amino-1-benzylpiperidine-4-carbonitrile)

4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5) belongs to anime. Nitrous acid converts secondary amines (aliphatic or aromatic) to N-nitroso compounds (nitrosamines): R2NH + HNO2 → R2N―NO. Some nitrosamines are potent cancer-inducing substances, and their possible formation is a serious consideration when nitrites, which are salts of nitrous acid, are present in foods or pharmaceutical preparations. Tertiary amines give rise to nitrosamines more slowly; an alkyl group is eliminated as an aldehyde or ketone, along with nitrous oxide, N2O.Application In Synthesis of 4-Amino-1-benzylpiperidine-4-carbonitrile

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Metwally, Kamel A.; Dukat, Malgorzata; Egan, Christina T.; Smith, Carol; DuPre, Ann; Gauthier, Colleen B.; Herrick-Davis, Katharine; Teitler, Milt; Glennon, Richard A. published their research in Journal of Medicinal Chemistry on December 3 ,1998. The article was titled 《Spiperone: Influence of Spiro Ring Substituents on 5-HT2A Serotonin Receptor Binding》.Recommanded Product: 136624-42-5 The article contains the following contents:

Spiperone is a widely used pharmacol. tool that acts as a potent dopamine D2, serotonin 5-HT1A, and serotonin 5-HT2A antagonist. Although spiperone also binds at 5-HT2C receptors, it is one of the very few agents that display some (∼1000-fold) binding selectivity for 5-HT2A vs. 5-HT2C receptors and, hence, might serve as a useful template for the development of novel 5-HT2A antagonists if the impact of its various substituent groups on binding was known. In the present investigation we focused on the 1,3,8-triazaspiro[4.5]decanone portion of spiperone and found that replacement of the N1-Ph group with a Me group only slightly decreased affinity for cloned rat 5-HT2A receptors. However, N1-Me derivatives displayed significantly reduced affinity for 5-HT1A, 5-HT2C, and dopamine D2 receptors. Several representative examples were shown to behave as 5-HT2 antagonists. As such, N1-alkyl analogs of spiperone may afford entry into a novel series of 5-HT2A-selective antagonists. The experimental process involved the reaction of 4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5Recommanded Product: 136624-42-5)

4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5) belongs to anime. Examples of direct uses of amines and their salts are as corrosion inhibitors in boilers and in lubricating oils (morpholine), as antioxidants for rubber and roofing asphalt (diarylamines), as stabilizers for cellulose nitrate explosives (diphenylamine), as protectants against damage from gamma radiation (diarylamines), as developers in photography (aromatic diamines), as flotation agents in mining, as anticling and waterproofing agents for textiles, as fabric softeners, in paper coating, and for solubilizing herbicides.Recommanded Product: 136624-42-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

COA of Formula: C13H17N3On May 1, 2007 ,《Identification of a novel class of succinyl-nitrile-based Cathepsin S inhibitors》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Bekkali, Younes; Thomson, David S.; Betageri, Raj; Emmanuel, Michel J.; Hao, Ming-Hong; Hickey, Eugene; Liu, Weimin; Patel, Usha; Ward, Yancey D.; Young, Erick R. R.; Nelson, Richard; Kukulka, Alison; Brown, Maryanne L.; Crane, Kathy; White, Della; Freeman, Dorothy M.; Labadia, Mark E.; Wildeson, Jessi; Spero, Denice M.. The article conveys some information:

The synthesis and in vitro activities of a series of succinyl-nitrile-based inhibitors of Cathepsin S I [R1 = cyclohexyl, 4-methylcyclohexyl, 2-indanyl, etc.; R2 = H, R3 = PhCH2CH2, PhCH2OCH2, 4-ClC6H4CH2OCH2; R2R3 = CH2CH2, (CH2)2N(cyclo-C6H11)CH2, (CH2)2NMe(CH2)2, etc.] are described. Several members of this class show nanomolar inhibition of the target enzyme as well as cellular potency. The inhibitors displaying the greatest potency contain N-alkyl-substituted piperidine and pyrrolidine rings spiro-fused to the α-carbon of the P1 residue. In the part of experimental materials, we found many familiar compounds, such as 4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5COA of Formula: C13H17N3)

4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5) belongs to anime. The reaction of alkyl halides, R―X, where X is a halogen, or analogous reagents with ammonia (or amines) is useful with certain compounds. Not all alkyl halides are effective reagents; the reaction is sluggish with secondary alkyl groups and fails with tertiary ones. Its usefulness is largely confined to primary alkyl halides (those having two hydrogen atoms on the reacting site).COA of Formula: C13H17N3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Chaturvedula, Prasad V.; Pin, Sokhom; Tholady, George; Conway, Charlie M.; Macor, John E.; Dubowchik, Gene M. published an article in Bioorganic & Medicinal Chemistry Letters. The title of the article was 《Design and synthesis of potent antagonists containing rigid spirocyclic privileged structures for the CGRP receptor》.Name: 4-Amino-1-benzylpiperidine-4-carbonitrile The author mentioned the following in the article:

We report the synthesis of rigid spirocyclic systems as conformationally constrained variants of the Ala-Phe-NH2 dipeptide amide C-terminus of the calcitonin gene-related peptide (CGRP). CGRP receptor antagonists containing these moieties displayed potent affinity, functional antagonism and excellent oxidative stability. Structure-activity relationship studies demonstrated the relative importance of hydrogen bond donor/acceptor functionalities and the preferred orientation of an aromatic ring. Antagonists showed potent and full reversal of CGRP-induced dilation of ex vivo human intracranial arteries.4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5Name: 4-Amino-1-benzylpiperidine-4-carbonitrile) was used in this study.

4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5) belongs to anime. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Name: 4-Amino-1-benzylpiperidine-4-carbonitrile

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Quality Control of 4-Amino-1-benzylpiperidine-4-carbonitrileOn May 1, 2007 ,《Identification of a novel class of succinyl-nitrile-based Cathepsin S inhibitors》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Bekkali, Younes; Thomson, David S.; Betageri, Raj; Emmanuel, Michel J.; Hao, Ming-Hong; Hickey, Eugene; Liu, Weimin; Patel, Usha; Ward, Yancey D.; Young, Erick R. R.; Nelson, Richard; Kukulka, Alison; Brown, Maryanne L.; Crane, Kathy; White, Della; Freeman, Dorothy M.; Labadia, Mark E.; Wildeson, Jessi; Spero, Denice M.. The article conveys some information:

The synthesis and in vitro activities of a series of succinyl-nitrile-based inhibitors of Cathepsin S I [R1 = cyclohexyl, 4-methylcyclohexyl, 2-indanyl, etc.; R2 = H, R3 = PhCH2CH2, PhCH2OCH2, 4-ClC6H4CH2OCH2; R2R3 = CH2CH2, (CH2)2N(cyclo-C6H11)CH2, (CH2)2NMe(CH2)2, etc.] are described. Several members of this class show nanomolar inhibition of the target enzyme as well as cellular potency. The inhibitors displaying the greatest potency contain N-alkyl-substituted piperidine and pyrrolidine rings spiro-fused to the α-carbon of the P1 residue. In the part of experimental materials, we found many familiar compounds, such as 4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5Quality Control of 4-Amino-1-benzylpiperidine-4-carbonitrile)

4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5) belongs to anime. The reaction of alkyl halides, R―X, where X is a halogen, or analogous reagents with ammonia (or amines) is useful with certain compounds. Not all alkyl halides are effective reagents; the reaction is sluggish with secondary alkyl groups and fails with tertiary ones. Its usefulness is largely confined to primary alkyl halides (those having two hydrogen atoms on the reacting site).Quality Control of 4-Amino-1-benzylpiperidine-4-carbonitrile

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Chaturvedula, Prasad V.; Pin, Sokhom; Tholady, George; Conway, Charlie M.; Macor, John E.; Dubowchik, Gene M. published an article in Bioorganic & Medicinal Chemistry Letters. The title of the article was 《Design and synthesis of potent antagonists containing rigid spirocyclic privileged structures for the CGRP receptor》.Related Products of 136624-42-5 The author mentioned the following in the article:

We report the synthesis of rigid spirocyclic systems as conformationally constrained variants of the Ala-Phe-NH2 dipeptide amide C-terminus of the calcitonin gene-related peptide (CGRP). CGRP receptor antagonists containing these moieties displayed potent affinity, functional antagonism and excellent oxidative stability. Structure-activity relationship studies demonstrated the relative importance of hydrogen bond donor/acceptor functionalities and the preferred orientation of an aromatic ring. Antagonists showed potent and full reversal of CGRP-induced dilation of ex vivo human intracranial arteries.4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5Related Products of 136624-42-5) was used in this study.

4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5) belongs to anime. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Related Products of 136624-42-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem