672295-87-3

Upstream product

• 110-89-4 piperidine 
• 626-19-7 Isophthalaldehyde 
• 13290-48-7 3-methylphenyl(piperidin-1-yl)methanone 
• 87199-16-4 3-Formylphenylboronic acid 
• 1013-92-9 di(piperidin-1-yl)methanethione 
• 619-21-6 m-formylphenyl benzoic acid 

Downstream Products

• 748771-96-2 (3-{[2-(3-isopropoxy-phenylamino)-ethylamino]-methyl}-phenyl)-piperidin-1-yl-methanone 
• 748771-93-9 (3-{[2-(2-isopropoxy-phenylamino)-ethylamino]-methyl}-phenyl)-piperidin-1-yl-methanone 
• 748772-24-9 [2-(2-methanesulfonylamino-phenylamino)-ethyl]-[3-(piperidine-1-carbonyl)-benzyl]-carbamic acid tert-butyl ester 
• 748772-48-7 {2-[(2-isopropoxy-phenyl)-methyl-amino]-ethyl}-[3-(piperidine-1-carbonyl)-benzyl]-carbamic acid tert-butyl ester 
• 748772-23-8 [2-(2-isopropylamino-phenylamino)-ethyl]-[3-(piperidine-1-carbonyl)-benzyl]-carbamic acid tert-butyl ester 
• 748772-21-6 [2-(2-nitro-phenylamino)-ethyl]-[3-(piperidine-1-carbonyl)-benzyl]-carbamic acid tert-butyl ester 
• 748772-22-7 [2-(2-amino-phenylamino)-ethyl]-[3-(piperidine-1-carbonyl)-benzyl]-carbamic acid tert-butyl ester 
• 748772-46-5 [2-(2-isopropoxy-phenylamino)-ethyl]-[3-(piperidine-1-carbonyl)-benzyl]-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

Palladium-Catalyzed Desulfurative Amide Formation from Thioureas and Arylboronic Acids

The development of the reactivity on carbene complexes would lead to the creation of novel synthetic strategies. We discovered herein the Pd-catalyzed desulfurative amide formation involved Suzuki-Miyaura coupling reaction, notably the Pd complex was generated in situ from thioureas, Ag salt and Pd catalyst. Silver salt was essential for the construction of this type of carbenes from available and stable thioureas and well participated in the catalytic cycle. We report a method for the synthesis of arylamides from arylboronic acids, which greatly enriched the application of thiourea chemistry and expanded the application of the Suzuki-Miyaura coupling.

(Z)-3-(3-formyl benzylidene) piperazinedione type compound and application thereof to preparation of anti-tumor medicine

The invention discloses a (Z)-3-(3-formyl benzylidene) piperazinedione type compound and application thereof to preparation of anti-tumor medicine. In a general formula (I) shown as the accompanying drawing, Rl is selected from substituted or nonsubstituted saturated nitrogen-containing multivariate heterocycles, substituted or nonsubstituted unsaturated sulfur-containing multivariate heterocycles, and substituted or nonsubstituted unsaturated oxygen containing multivariate heterocycles, and the multivariate heterocycles are 4 to 6 membered heterocycles. R2 is 5-tertiary butyl-1H-imidazole or pyridine. The invention also discloses a purpose of the compound to preparation of medicine composition aspects for treating tumor diseases, particularly, purposes to preparation of medicine compositions for treating pancreatic cancer and/or lung cancer aspects.

Design, synthesis and biological evaluation of anti-pancreatic cancer activity of plinabulin derivatives based on the co-crystal structure

Based on the co-crystal structures of tubulin with plinabulin and Compound 1 (a derivative of plinabulin), a total of 18 novel plinabulin derivatives were designed and synthesized. Their biological activities were evaluated against human pancreatic cancer BxPC-3 cell lines. Two novel Compounds 13d and 13e exhibited potent activities with IC50 at 1.56 and 1.72 nM, respectively. The tubulin polymerization assay indicated that these derivatives could inhibit microtubule polymerization. Furthermore, the interaction between tubulin and these compounds were elucidated by molecular docking. The binding modes of Compounds 13d and 13e were similar to the co-crystal structure of Compound 1. H-π interaction was observed between the aromatic hydrogen of thiophene moiety with Phe20, which could enhance their binding affinities.

Development of a Rhodium(II)-Catalyzed Chemoselective C(sp3)-H Oxygenation

We report the first example of RhII-catalyzed chemoselective double C(sp3)-H oxygenation, which can directly transform various toluene derivatives into highly valuable aromatic aldehydes with great chemoselectivity and practicality. The critical combination of catalyst Rh(OAc)2, oxidant Selectfluor, and solvents of TFA/TFAA promises the successful delivery of the oxidation with satisfactory yields. A possible mechanism involving a unique carbene-Rh complex is proposed, and has been supported by both experiments and theoretical calculations.

Metal-free one-pot synthesis of amides using graphene oxide as an efficient catalyst

Graphene oxide (GO), exhibiting a high degree of oxygen functionality and various structural defects, was found to be a highly efficient and cost effective carbocatalyst for the one-pot base-free synthesis of amides from aromatic aldehydes and secondary amine. The chemical and structural features of GO, as probed by FTIR, Raman, XRD and HRTEM analyses, were discussed to understand the catalytic mechanism for the synthesis of amides. The present method obviates the use of transition metal catalysts and needs shorter reaction time. This journal is

Metal-free one-pot synthesis of amides using graphene oxide as an efficient catalyst

Graphene oxide (GO), exhibiting a high degree of oxygen functionality and various structural defects, was found to be a highly efficient and cost effective carbocatalyst for the one-pot base-free synthesis of amides from aromatic aldehydes and secondary amine. The chemical and structural features of GO, as probed by FTIR, Raman, XRD and HRTEM analyses, were discussed to understand the catalytic mechanism for the synthesis of amides. The present method obviates the use of transition metal catalysts and needs shorter reaction time. This journal is

Gold-catalyzed amide synthesis from aldehydes and amines in aqueous medium

An efficient gold-catalyzed amide synthesis from aldehydes and amines in aqueous medium under mild reaction conditions has been developed.

Aryl piperidine amides

The invention provides novel GlyT2 inhibiting compounds useful in modulating, treating, or preventing: anxiolytic disorders; a condition requiring treatment of injured mammalian nerve tissue; a condition amenable to treatment through administration of a neurotrophic factor; a neurological disorder; or obesity; an obesity-related disorder.

Inhibitors of the glycine transporter type-2 (GlyT-2): synthesis and biological activity of benzoylpiperidine derivatives.

A series of benzoylpiperidine analogs related to 4a was prepared, and their ability to inhibit the uptake of [(14)C]-glycine in COS7 cells transfected with human glycine transporter type-2 (GlyT-2) was evaluated. Small structural changes to the benzoylpiperidine region of the molecule led to a significant decrease in GlyT-2 inhibitory activity. In contrast, the distal aryl ring was more tolerant to functional group modifications and could accommodate a variety of substitutes at the C-2 or C-3 positions. Comparable activities to 4a were obtained by replacing the anilino nitrogen with an ether linkage 27 or by exchanging the isopropoxy ether moiety with an isopropyl amino group 15. A distinct preference for a 2-carbon tether (n=1) was observed relative to the corresponding 3-carbon homolog (n=2).