140695-85-8

Usage

Uses

(R)-(-)-1-Boc-3-(hydroxymethyl)piperidine is used as pharmaceutical intermediate.

Upstream product

• 116574-71-1 (±)-tert-butyl 3-(hydroxymethyl)piperidine-1-carboxylate 
• 140645-20-1 t-butyl (R,S)-3-<(butyryloxy)methyl>-1-piperidine-carboxylate 
• 140695-98-3 (R)-3-Butyryloxymethyl-piperidine-1-carboxylic acid tert-butyl ester 
• 24424-99-5 di-tert-butyl dicarbonate 
• 37675-20-0 (R)-3-hydroxymethyl piperidine 
• 108-05-4 vinyl acetate 
• 163438-09-3 (R)-1-Boc-nipecotic acid 
• 109-02-4 4-methyl-morpholine 
• 498-95-3 (R)-nipecotic acid 
• 33741-15-0 methyl (4E)-hepta-4,6-dienoate 
• 79280-39-0 (4E)-hepta-4,6-dienal 
• 651321-53-8 Benzyl-[(E)-hepta-4,6-dien-(E)-ylidene]-amine 
• 445398-78-7 N-benzyl-hepta-4(E),6-dien-1-amine 
• 194726-46-0 (3R)-3-formylpiperidine-1-carboxylic acid tert-butyl ester 

Downstream Products

• 384830-08-4 tert-butyl (3R)-3-(iodomethyl) piperidine-1-carboxylate 
• 191092-07-6 (R)-tert-butyl 3-((tosyloxy)methyl)piperidine-1-carboxylate 
• 384830-09-5 (S)-3-((2S,3R)-2-Benzyloxycarbonyl-4-oxo-azetidin-3-ylmethyl)-piperidine-1-carboxylic acid tert-butyl ester 
• 384830-10-8 (2S,3R)-3-((S)-1-{Benzyloxycarbonylamino-[(E)-benzyloxycarbonylimino]-methyl}-piperidin-3-ylmethyl)-4-oxo-azetidine-2-carboxylic acid benzyl ester 
• 384830-11-9 (2S,3R)-3-((S)-1-{Benzyloxycarbonylamino-[(E)-benzyloxycarbonylimino]-methyl}-piperidin-3-ylmethyl)-4-oxo-1-[4-(6-phenyl-hexanoyl)-piperazine-1-carbonyl]-azetidine-2-carboxylic acid benzyl ester 
• 1002359-91-2 tert-butyl (3R)-3-(bromomethyl)piperidine-1-carbamate 
• 205194-11-2 (R)-3-hydroxymethyl-1-methylpiperidine 
• 1246289-49-5 C₁₈H₂₀Cl₂N₂O 
• 158406-99-6 1,1-dimethylethyl (3S)-3-(bromomethyl)-1-piperidinecarboxylate 
• 1381949-89-8 C₂₃H₃₂ClF₃N₄O₃ 
• 1381949-88-7 C₂₂H₃₂ClFN₄O₃ 

Relevant academic research and scientific papers

Design and evaluation of novel piperidine HIV-1 protease inhibitors with potency against DRV-resistant variants

A novel class of HIV-1 protease inhibitors with flexible piperidine as the P2 ligand was designed with the aim of improving extensive interactions with the active subsites. Many inhibitors exhibited good to excellent inhibitory effect on enzymatic activity and viral infectivity. In particular, inhibitor 3a with (R)-piperidine-3-carboxamide as the P2 ligand and 4-methoxybenzenesulfonamide as the P2’ ligand showed an enzyme Ki value of 29 pM and antiviral IC50 value of 0.13 nM, more than six-fold enhancement of activity compared to DRV. Furthermore, there was no significant change in potency against DRV-resistant mutations and HIV-1NL4?3 variant for 3a. Besides, inhibitor 3a exhibited potent antiviral activity against subtype C variants with low nanomole EC50 values. In addition, the molecular modeling revealed important hydrogen bonds and other favorable van der Waals interactions with the backbone atoms of the protease and provided insight for designing and optimizing more potent HIV-1 protease inhibitors.

Palladium-catalyzed ring-closing reaction via C-N bond metathesis for rapid construction of saturated N-heterocycles

The ring-closing reactions based on chemical bond metathesis enable the efficient construction of a wide variety of cyclic systems which receive broad interest from medicinal and organic communities. However, the analogous reaction with C-N bond metathesis as a strategic fundamental step remains an unanswered challenge. Herein, we report the design of a new fundamental metallic C-N bond metathesis reaction that enables the palladium-catalyzed ring-closing reaction of aminodienes with aminals. The reactions proceed efficiently under mild conditions and exhibit broad substrate generality and functional group compatibility, leading to a wide variety of 5- to 16-membered N-heterocycles bearing diverse frameworks and functional groups.

SUBSTITUTED (PIPERIDIN-1-YL)ARYL ANALOGUES FOR MODULATING AVILACTIVITY

In one aspect, the disclosure relates to compounds useful to regulate, limit, or inhibit the expression of AVIL (advillin), methods of making same, pharmaceutical compositions comprising same, and methods of treating disorders associated with AVIL dysregulation using same. In aspects, the disclosed compounds, compositions and methods are useful for treating disorders or diseases in which the regulation, limitation, or inhibition of the expression of AVIL can be clinically useful, such as, for example, the treatment of cancer. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

Synthetic method for (R)-N-tert-butoxycarbonyl-3-hydroxymethylpiperidine

The invention discloses a synthetic method for (R)-N-tert-butoxycarbonyl-3-hydroxymethylpiperidine. The method comprises the following four steps: synthesizing ethyl 3-piperidinecarboxylate (compoundII), synthesizing ethyl (R)-nipecotate-L-tartarate (compound III), synthesizing ethyl (R)-N-Boc-3-piperidinecarboxylate (compound IV) and synthesizing the (R)-N-tert-butoxycarbonyl-3-hydroxymethylpiperidine (compound V); and the method comprises the following special steps: synthesizing the compound II by using 3-piperidinecarboxylic acid (compound I) as a raw material through chloroacylation andethanol esterification; performing a salt formation reaction to form the compound III; adding a Boc anhydride and performing a reaction to obtain the compound IV; and finally performing sodium borohydride reduction to obtain the compound V. The method provided by the invention has the advantages of mild reaction conditions, environmental friendliness, simple operation steps, better reproducibilityand high practicability, and is suitable for industrial mass production of the (R)-N-tert-butoxycarbonyl-3-hydroxymethylpiperidine.

KRAS G12C INHIBITORS

The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.

KRAS G12C INHIBITORS

The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.

COMPOUNDS USEFUL AS KINASE INHIBITORS

This invention relates to novel compounds. The compounds of the invention are tyrosine kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Bruton's tyrosine kinase (BTK).The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of Bruton's tyrosine kinase, for example cancer, lymphoma, leukemia and immunological diseases.

Benzimidazole-2-piperazine compound, its pharmaceutical composition and its preparation and use

The invention relates to a benzimidazole-2-piperazine derivative and a preparing method and application of the benzimidazole-2-piperazine derivative in medicine, in particular to a novel benzimidazole-2-piperazine derivative shown in the general formula (I), a preparing method of the derivative, a pharmaceutical composition containing the derivative and application of the derivative serving as a therapeutic agent, especially serving as a poly (ADP-ribose) polymerase (PARP) inhibitor. In the general formula (I), R refers to hydrogen or halogen, G refers to carbonyl or methylene, m is 1-2, n is 1-3, and Q refers to hydrogen or C1-C4 alkyl. When X is methylene and Y is NR1 or methylene, X is NR1; R1 refers to hydrogen, C1-C6 alkyl, benzyl, COR2 or SO2R2; R2 refers to the following groups which are not substituted or groups substituted by 1-3 substituent groups, including C1-C6 alkyl, C3-C8 naphthenic base, phenyl, benzyl, naphthyl and C5-C10 aromatic heterocycle base, heterocycle in the C5-C10 aromatic heterocycle base comprises 1-3 heteroatoms selected from N, O and S, and the substituent groups are selected from the following atoms or groups of C1-C6 alkyl, C1-C6 alkoxy, halogen, amidogen, nitryl, sulfydryl, hydroxyl, cyanogroup and trifluoromethyl. The general formula (I) is shown in the specification.

4-Piperidines and 3-pyrrolidines as dual serotonin and noradrenaline reuptake inhibitors: Design, synthesis and structure-activity relationships

Single enantiomer [(aryloxy)(pyridinyl)methyl]piperidine and pyrrolidine derivatives 5-9 are inhibitors of monoamine reuptake. Structure-activity relationships established that monoamine reuptake inhibition are functions of amine, pyridine isomer, aryloxy ring substitution and stereochemistry. Consequently, selective NRIs, selective SRIs, dual SNRIs and triple SNDRIs were all identified. Dual SNRIs 5l-a and 9c were evaluated in additional pharmacology and pharmacokinetic studies as representative examples from this series.

BISARYLUREA DERIVATIVES USEFUL FOR INHIBITING CHK1

Aryl- and heteroaryl-substituted urea compounds useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division also are disclosed. Formula (I).