220394-97-8

Usage

Uses

Used in Pharmaceutical Industry:
1-BOC-4-CBZ-AMINO-PIPERIDINE is used as a key intermediate for the synthesis of various pharmaceuticals due to its ability to contribute to the development of biologically active molecules. Its role in creating a wide range of compounds makes it invaluable in the production of medications that address diverse health conditions.
Used in Agrochemical Industry:
In the agrochemical sector, 1-BOC-4-CBZ-AMINO-PIPERIDINE is utilized as a building block for the synthesis of compounds that have applications in crop protection and other agricultural chemicals. Its versatility allows for the creation of molecules that can be tailored to specific needs within this industry.
Used in Fine Chemicals Production:
1-BOC-4-CBZ-AMINO-PIPERIDINE is also used in the production of fine chemicals, where its unique properties are leveraged to create specialty compounds for various applications, including but not limited to research, fragrances, and other high-value chemical products.
Given the sensitivity of 1-BOC-4-CBZ-AMINO-PIPERIDINE to air and moisture, it is crucial that it is handled and stored properly to maintain its integrity and ensure the quality of the end products in which it is used.

InChI:InChI=1/C18H26N2O4/c1-18(2,3)24-17(22)20-11-9-15(10-12-20)19-16(21)23-13-14-7-5-4-6-8-14/h4-8,15H,9-13H2,1-3H3,(H,19,21)

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 84358-13-4 N-[(tert-butoxy)carbonyl]piperidine-4-carboxylic acid 
• 100-51-6 benzyl alcohol 
• 87120-72-7 1-(tert-butoxycarbonyl)-4-aminopiperidine 
• 124443-68-1 1-tert-Butyl 4-methyl piperidine-1,4-dicarboxylate 
• 91419-48-6 4-carbamoyl-piperidine-1-carboxylic acid tert-butyl ester 
• 180695-80-1 tert-butyl 4-azidopiperidine-1-carboxylate 
• 180695-79-8 tert-butyl 4-bromo-1-piperidinecarboxylate 
• 90633-18-4 4-bromo-1H-piperidine 
• 501-53-1 benzyl chloroformate 

Downstream Products

• 235420-64-1 4-(allyl-benzyloxycarbonyl-amino)-piperidine-1-carboxylic acid tert-butyl ester 
• 847039-05-8 4-(((benzyloxy)carbonyl)(methyl)amino)piperidine-1-carboxylic acid tert-butyl ester 
• 220394-98-9 4-(benzyloxycarbonyl-propyl-amino)-piperidine-1-carboxylic acid tert-butyl ester 
• 182223-54-7 piperidin-4-ylcarbamic acid benzyl ester 
• 1427058-43-2 benzyl N-[1-(2-fluoropentyl)piperidin-4-yl]carbamate 
• 1427058-31-8 2-[(3S,4R)-1-{[2-chloro-6-(trifluoromethyl)phenyl]methyl}-3-{[1-(2-fluoropentyl)piperidin-4-yl]carbamoyl}-4-methylpyrrolidin-3-yl]acetic acid 
• 1427309-25-8 tert-butyl 2-[(3S,4R)-1-benzyl-3-{[1-(2-fluoropentyl)piperidin-4-yl]carbamoyl}-4-methylpyrrolidin-3-yl]acetate 
• 1427309-26-9 tert-butyl 2-[(3S,4R)-1-{[2-chloro-6-(trifluoromethyl)phenyl]methyl}-3-{[1-(2-fluoropentyl)piperidin-4-yl]carbamoyl}-4-methylpyrrolidin-3-yl]acetate 
• 207296-89-7 piperidin-4-ylcarbamic acid benzyl ester hydrochloride 
• 609804-23-1 benzyl (1-iso-propylpiperidin-4-yl)carbamate 

Relevant academic research and scientific papers

COMPOUND WITH ANTICANCER ACTIVITY

A compound having anticancer activity, or a pharmaceutically acceptable salt thereof is provided. Used is a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: (wherein, L1 and L2 are the same or different and each represents a group represented by one formula selected from the group consisting of formulas (A) to (F), and S represents a group represented by one formula selected from the group consisting of formulas (S1) to (S18)).

Carbamate Synthesis Using a Shelf-Stable and Renewable C1 Reactant

4-Propylcatechol carbonate is a shelf-stable, renewable C1 reactant. It is easily prepared from renewable 4-propylcatechol (derived from wood) and dimethyl carbonate (derived from CO2) using a reactive distillation system. In this work, the 4-propylcatechol carbonate is used for the two-step synthesis of carbamates under mild reaction conditions. In the first step, 4-propylcatechol carbonate is treated with an alcohol at 50–80 °C in the presence of a Lewis acid catalyst, such as Zn(OAc)2?2 H2O. With liquid alcohols, no solvent is used and with solid alcohols 2-methyltetrahydrofuran is used as solvent. In the second step, the alkyl 2-hydroxy-propylphenyl carbonate intermediates obtained react with amines at room temperature in 2-methyltetrahydrofuran, forming the target carbamates and the byproduct 4-propylcatechol, which can be recycled into a carbonate reactant.

Discovery of 2-substituted 1H-benzo[d]immidazole-4-carboxamide derivatives as novel poly(ADP-ribose)polymerase-1 inhibitors with in?vivo anti-tumor activity

Novel 1H-benzo[d]immidazole-4-carboxamide derivatives bearing five-membered or six-membered N-heterocyclic moieties at the 2-position were designed and synthesized as PARP-1 inhibitors. Structure-activity relationships were conducted and led to a number of potent PARP-1 inhibitors having IC50 values in the single or double digit nanomolar level. Some potent PARP-1 inhibitors also had similar inhibitory activities against PARP-2. Among all the synthesized compounds, compound 10a and 11e displayed strong potentiation effects on temozolomide (TMZ) in MX-1?cells (PF50?=?7.10, PF50?=?4.17). In?vivo tumor growth inhibition was investigated using compound 10a in combination with TMZ, and it was demonstrated that compound 10a could strongly potentiate the cytotoxicity of TMZ in MX-1 xenograft tumor model. Two co-crystal structures of compounds 11b and 15e complexed with PARP-1 were achieved and demonstrated a unique binding mode of these benzo-imidazole derivatives.

AMIDINE COMPOUND AND BACTERICIDAL AGENT

PROBLEM TO BE SOLVED: To provide a novel amidine compound excellent in bactericidal property and safety and capable of being industrially advantageously synthesized and a bactericidal agent or plant disease control agent containing the amidine compound as an active ingredient. SOLUTION: There is provided a compound represented by the formula [I] or a salt hereof. [I], where Y is an unsubstituted/substituted bivalent cyclic amine residue, X and Z are each independently an unsubstituted/substituted alkylene group or the like, W is a singe bond or -N(R5)-, R5 is H, an unsubstituted/substituted heterocycle group or the like, R1 to R3 are each independently H, an unsubstituted/substituted hydrocarbon group or the like, A is an aryl group or a heteroaryl group substituted by carboxy amidine. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT

2,4-disubstituted [...] compound, and its preparation, and pharmaceutical composition and use thereof

The invention discloses new 2,4-disubstituted quinazoline compounds and a preparation method, a medicinal composition and application thereof. The invention particularly relates to 2,4-disubstituted quinazoline compounds shown as a general formula I, medicinal salts thereof, precursors or derivatives thereof with the same biological function, a preparation method thereof, a composition containing one or more of the compounds, and application of the compounds in inhibiting activity of Pin1 enzyme, inhibiting activity of tumor growth and the like.

Identification of novel aminopiperidine derivatives for antibacterial activity against Gram-positive bacteria

We have previously reported amidopiperidine derivatives as a novel peptide deformylase (PDF) inhibitor and evaluated its antibacterial activity against Gram-positive bacteria, but poor pharmacokinetic profiles have resulted in low efficacy in in vivo mouse models. In order to overcome these weaknesses, we newly synthesized aminopiperidine derivatives with remarkable antimicrobial properties and oral bioavailability, and also identified their in vivo efficacy against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus (VRE) and penicillin-resistant Streptococcus pneumoniae (PRSP).

Hofmann Rearrangement of Carboxamides Mediated by N-Bromoacetamide

An efficient, one-pot procedure for the Hofmann rearrangement of aromatic and aliphatic amides has been developed. Methyl and benzyl carbamates are produced with N-bromoacetamide in the presence of lithium hydroxide or lithium methoxide, in high yields. β-Phenylamino amides gave five-membered cyclic ureas stereospecifically. Side products of aryl or benzyl bromination were minimized. This procedure offers an easy access to various protected amines or diamines, which represent important synthetic precursors.

INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7)

The present invention provides novel compounds of Formula (I) and Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g.,leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject. (I)

BENZAMIDE CGRP RECEPTOR ANTAGONISTS

The present invention is directed to benzamide compounds which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

PYRROLIDINE-3-YLACETIC ACID DERIVATIVE

A compound represented by formula (1) or a pharmaceutically acceptable salt thereof has an inhibitory effect in the fractalkine-CX3CR1 pathway: wherein R represents a C1-6 alkyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group A, a C3-8 cycloalkyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group A, or a C3-8 cycloalkenyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group A, X represents a C1-6 alkyl group, Y and Z are the same or different from each other and each represents a halogen atom or a C1-6 alkyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group B, n represents 0 or 1, Substituent Group A consists of halogen atoms, and Substituent Group B consists of halogen atoms.