158144-82-2

Basic information

• Product Name: 1-N-BOC-4-AMINOMETHYL-4-PHENYLPIPERIDINE
• Synonyms: 1-N-BOC-4-AMINOMETHYL-4-PHENYLPIPERIDINE;4-Aminomethyl-4-phenylpiperidin-1-carboxylic acid tert-butyl ester;tert-butyl 4-(aminomethyl)-4-phenylpiperidine-1-carboxylate;1-Piperidinecarboxylic acid, 4-(aminomethyl)-4-phenyl-, 1,1-dimethylethyl ester
• CAS NO: 158144-82-2
• Molecular Formula: C₁₇H₂₆N₂O₂
• Molecular Weight: 290.4
• EINECS: 604-604-1
• Mol File: 158144-82-2.mol

Chemical Properties

• Melting Point: 64℃
• Boiling Point: 402.698 °C at 760 mmHg
• Flash Point: 197.345 °C
• Appearance: /
• Density: 1.067 g/cm³
• Storage Temp.: 2-8°C
• PKA: 10.13±0.29(Predicted)
• CAS DataBase Reference: 1-N-BOC-4-AMINOMETHYL-4-PHENYLPIPERIDINE(CAS DataBase Reference)
• NIST Chemistry Reference: 1-N-BOC-4-AMINOMETHYL-4-PHENYLPIPERIDINE(158144-82-2)
• EPA Substance Registry System: 1-N-BOC-4-AMINOMETHYL-4-PHENYLPIPERIDINE(158144-82-2)

Safety Data

• Hazardous Substances Data: 158144-82-2(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Research:
1-N-BOC-4-AMINOMETHYL-4-PHENYLPIPERIDINE is used as a precursor in the synthesis of bioactive compounds for pharmaceutical research. Its BOC protecting group allows for mild deprotection conditions, revealing the free amine, which is crucial for the development of new therapeutic agents.
Used in Medicinal Chemistry:
In the field of medicinal chemistry, 1-N-BOC-4-AMINOMETHYL-4-PHENYLPIPERIDINE is utilized as a versatile starting material for the creation of new therapeutic agents. Its unique structure and functional groups enable the design and synthesis of compounds with potential applications in the treatment of various diseases and conditions.
Used in Drug Development:
1-N-BOC-4-AMINOMETHYL-4-PHENYLPIPERIDINE is employed as a key intermediate in drug development, where its chemical properties and reactivity can be harnessed to produce novel pharmaceutical drugs with improved efficacy and safety profiles.
Used in Chemical Synthesis:
In chemical synthesis, 1-N-BOC-4-AMINOMETHYL-4-PHENYLPIPERIDINE serves as a building block for the preparation of complex organic molecules and pharmaceutical intermediates, contributing to the advancement of synthetic chemistry and the discovery of new chemical entities.
Used in Drug Discovery:
1-N-BOC-4-AMINOMETHYL-4-PHENYLPIPERIDINE is used as a scaffold in drug discovery, where its structural features can be modified to explore new chemical space and identify potential drug candidates with novel mechanisms of action.
Used in Bioactive Compounds Synthesis:
In the synthesis of bioactive compounds, 1-N-BOC-4-AMINOMETHYL-4-PHENYLPIPERIDINE is utilized as a key component, providing a foundation for the development of molecules with potential biological activities and therapeutic properties.

Upstream product

• 40481-13-8 4-phenyl-4-cyanopiperidine 
• 24424-99-5 di-tert-butyl dicarbonate 
• 71999-74-1 tert-butyl N-(2-chloroethyl)carbamate 
• 140-29-4 phenylacetonitrile 
• 51304-58-6 4-cyano-4-phenylpiperidine hydrochloride 
• 158144-79-7 tert-butyl 4-cyano-4-phenylpiperidine-1-carboxylate 

Downstream Products

• 199104-96-6 4-(Methanesulfonylamino-methyl)-4-phenyl-piperidine-1-carboxylic acid tert-butyl ester 
• 158144-81-1 4-[(2-Methoxy-benzylamino)-methyl]-4-phenyl-piperidine-1-carboxylic acid tert-butyl ester 
• 906369-80-0 4-[(2-nitro-benzenesulfonylamino)-methyl]-4-phenyl-piperidine-1-carboxylic acid tert-butyl ester 
• 312638-96-3 tert-butyl 4-(aminomethyl)-4-cyclohexylpiperidine-1-carboxylate 
• 1071483-40-3 tert-butyl 4-((3-fluoro-4-(2-(4-methylpyridin-2-ylamino)thiazol-5-ylthio)picolinamido)methyl)-4-phenylpiperidine-1-carboxylate 
• 1146362-37-9 tert.butyl 4-[(2-methoxyacetylamino)-methyl]-4-phenylpiperidine-1-carboxylate 
• 199104-98-8 tert-butyl 4-(acetylaminomethyl)-4-phenylpiperidine-1-carboxylate 
• 761355-17-3 (4-phenylpiperidin-4-yl)methanamine 
• 1071485-35-2 N-((1-(4-chloro-3-sulfamoylbenzoyl)-4-phenylpiperidin-4-yl)methyl)-3-fluoro-4-(2-(4-methylpyridin-2-ylamino)thiazol-5-ylthio)picolinamide hydrochloride 
• 1071485-37-4 N-((1-(1-aminocyclopropanecarbonyl)-4-phenylpiperidin-4-yl)methyl)-3-fluoro-4-(2-(4-methylpyridin-2-ylamino)thiazol-5-ylthio)picolinamide hydrochloride 
• 1071483-71-0 N-((1-(2-(dimethylamino)acetyl)-4-phenylpiperidin-4-yl)methyl)-3-fluoro-4-(2-(4-methylpyridin-2-ylamino)thiazol-5-ylthio)picolinamide hydrochloride 
• 1071484-39-3 3-fluoro-N-((1-(2-hydroxy-2-methylpropyl)-4-phenylpiperidin-4-yl)methyl)-4-(2-(4-methylpyridin-2-ylamino)thiazol-5-ylthio)picolinamide hydrochloride 
• 1071484-33-7 N-((1-(2-cyanoethyl)-4-phenylpiperidin-4-yl)methyl)-3-fluoro-4-(2-(4-methylpyridin-2-ylamino)thiazol-5-ylthio)picolinamide hydrochloride 
• 1071484-09-7 N-((1-(cyclopropylmethyl)-4-phenylpiperidin-4-yl)methyl)-3-fluoro-4-(2-(4-methylpyridin-2-ylamino)thiazol-5-ylthio)picolinamide hydrochloride 

Relevant articles and documents

PYRIMIDINE-FUSED CYCLIC COMPOUND, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF

Disclosed in the present disclosure are a pyrimidine-fused cyclic compound or a pharmaceutically acceptable salt, hydrate, prodrug, stereoisomer, solvate or isotope labeled compound thereof. Also provided in the present disclosure are a preparation method for the compound, a composition comprising the compound and a use of the compound for the preparation of a medicament for the prevention and/or treatment of a disease or condition associated with abnormal SHP2 activity.

HETEROCYCLIC COMPOUNDS, MEDICAMENTS CONTAINING SAID COMPOUNDS, USE THEREOF AND PROCESSES FOR THE PREPARATION THEREOF

The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, and the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.

Novel 4,4-disubstituted piperidine-based C-C chemokine receptor-5 inhibitors with high potency against human immunodeficiency virus-1 and an improved human ether-a-go-go related gene (hERG) profile

We recently described (J. Med. Chem. 2008, 51, 6538-6546) a novel class of CCR5 antagonists with strong anti-HIV potency. Herein, we detail SAR converting leads 1 and 2 to druglike molecules. The pivotal structural motif enabling this transition was the secondary sulfonamide substituent. Further finetuning of the substituent pattern in the sulfonamide paved the way to enhancing potency and bioavailability and minimizing hERG inhibition, resulting in discovery of clinical compound 122 (GSK163929).

THIAZOLYL COMPOUNDS USEFUL AS KINASE INHIBITORS

The invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula I thiazolyl compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's disease

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.

2-aryl indole derivatives and their use as therapeutic agents

The present invention relates compounds of the formula (I): wherein R1a, R1b; and R2 represent a variety of substituents; R3 represents an optionally substituted phenyl, biphenyl or naphthyl or heteroaryl group; R4 represents hydrogen, C1-6alkyl, carbonyl (=O), (CH2)pphenyl or a C1-2alkylene bridge across the piperidine ring; R5 and R6 each independently represent a variety of substituents; or R5 and R6 together are linked so as to form an optionally substituted 5-or 6-membered ring; X represents an oxygen or a sulfur atom, two hydrogen atoms, ═NH or ═N(C1-6alkyl); Y is a straight or branched C1-4alkylene, C2-4alkenylene or C2-4alkynylene chain; the dotted line represents an optional double bond; m is zero or an integer from 1 to 4; n is an integer from 1 to 4; and p is an integer from 1 to 4; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.

Serine derived NK1 antagonists 2: A pharmacophore model for arylsulfonamide binding

Modifications to the spirocyclic aryl sulfonamide portion of serine derived NK1 antagonists allow a partial pharmacophore model to be developed.

4,4-Disubstituted piperidine high-affinity NK1 antagonists: Structure- activity relationships and in vivo activity

Previously reported studies from these laboratories described the design of a novel series of high-affinity NK1 antagonists based on the 4,4- disubstituted piperidine ring system. Further structure-activity studies have now established that for high NK1 affinity the benzyl ether side chain must be 3,5-disubstituted and highly lipophilic, the optimal side chain being the 3,5-bis(trifluoromethyl)benzyl ether, 12 (hNK1 IC50 = 0.95 nM). Additional studies have shown that this class of NK1 antagonist tolerates a wider range of substituents on the piperidine nitrogen, including acyl (38) (hNK1 IC50 = 5.3 nM) and sulfonyl (39) (hNK1 IC50 = 5.7 nM) derivatives. Following preliminary pharmacokinetic analysis, two compounds (32 and 43) were selected for in vivo study in the resiniferotoxin-induced vascular leakage model, both showing excellent profiles (ID50 = 0.22 and 0.28 mg/kg, respectively).

4-aminomethyl/thiomethyl/sulfonylmethyl-4-phenylpiperdines as tachykinin receptor antagonists

The present invention is directed to compounds of the formula (I) STR1 wherein R1, R2, R3, R5, R6, R7, R8, m, n and X are defined herein, and pharmaceutically acceptable salts th