64018-20-8

Usage

InChI:InChI=1/C10H14N2O/c11-7-6-10(13)12-8-9-4-2-1-3-5-9/h1-5H,6-8,11H2,(H,12,13)

Upstream product

• 71273-81-9 tert-butyl (3-(benzylamino)-3-oxopropyl)carbamate 
• 100-46-9 benzylamine 
• 219803-84-6 (2-benzylcarbamoyl-ethyl)-carbamic acid 9H-fluoren-9-ylmethyl ester 

Downstream Products

• 852873-28-0 [(2R,3R,4R,5R,6R)-6-Azidomethyl-2-(2-benzylcarbamoyl-ethylcarbamoyl)-4,5-bis-methoxymethoxy-tetrahydro-pyran-3-yl]-carbamic acid 9H-fluoren-9-ylmethyl ester 
• 852873-25-7 {(2R,3R,4R,5R,6R)-2-(2-Benzylcarbamoyl-ethylcarbamoyl)-6-[(9H-fluoren-9-ylmethoxycarbonylamino)-methyl]-4,5-bis-methoxymethoxy-tetrahydro-pyran-3-yl}-carbamic acid tert-butyl ester 
• 944150-45-2 benzyl {[3-(benzylamino)-3-oxopropyl]amino}carbonothioyl carbamate 
• 43199-18-4 3-Isothiocyanatopropionylbenzylamid 
• 64261-94-5 2-(β-N-benzylcarbamoylethyl)amino-1-phenyl-ethanol 
• 885022-19-5 C₃₆H₃₁F₄N₅O₆S 
• 852873-26-8 C₅₇H₈₀N₆O₁₉ 
• 852873-29-1 {2-[6-azidomethyl-2-(2-benzylcarbamoyl-ethylcarbamoyl)-4,5-bis-methoxymethoxy-tetrahydro-pyran-3-ylcarbamoyl]-6-[(9H-fluoren-9-ylmethoxycarbonylamino)-methyl]-4,5-bis-methoxymethoxy-tetrahydro-pyran-3-yl}-carbamic acid tert-butyl ester 
• 944150-46-3 benzyl N-[3-(benzylamino)-3-oxopropyl]amino[(6-[(methylamino)carbonyl]-2-pyridylmethyl)amino]methylenecarbamate 
• 86886-29-5 (E)-N-(2-Benzylcarbamoyl-ethyl)-3-(2,4-dihydroxy-6-methyl-pyrimidin-5-yl)-acrylamide 

Relevant academic research and scientific papers

Methylene C(sp3)-H β,β′-Diarylation of Cyclohexanecarbaldehydes Promoted by a Transient Directing Group and Pyridone Ligand

A hindered β-amino amide transient directing group effects di-trans-arylation of cyclohexanecarbaldehydes. The amide N-substituents are shown to affect yield and can enhance the rate of arylation compared with the α-amino acid. Addition of a pyridone ligand further enhanced reactivity. The reaction is successful for a range of aryl iodides, and various substituted cyclohexane carboxaldehydes, providing functionalized products from simple feedstocks. A mechanism is proposed evoking a transient enamine.

Synthesis and DNA-cleaving activity of lactenediynes conjugated with DNA-complexing moieties

Lactenediynes are compounds characterized by the fusion of a β-lactam with a cyclodeca-3-ene-1,5-diyne. In this work the most promising members of this family have been activated by attaching a carbalkoxy or a carbamoyl group to the azetidinone nitrogen, and conjugated to various DNA-complexing moieties, either acting by intercalation or through groove binding. These conjugated artificial enediynes have been demonstrated to possess in vitro ability to produce single and double strand cleavage of plasmid DNA. As potency and capacity to induce double cut, they rank among the best simple enediyne analogues ever prepared. A thorough investigation was carried out in order to develop the best suited linkers for assembling these conjugates.

2-[3-[2-[(25)-2-cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl] -1,2,3,4-tetrahydroisoquinoline: A potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV

Dipeptidyl peptidase IV (DPP-IV) inhibitors are expected to become a new type of antidiabetic drugs. Most known DPP-IV inhibitors often resemble the dipeptide cleavage products, with a proline mimic at the P1 site. As off-target inhibitions of DPP8 and/or DPP9 have shown profound toxicities in the in vivo studies, it is important to develop selective DPP-IV inhibitors for clinical usage. To achieve this, a new class of 2-[3-[[2-[(2S)-2-cyano-1-pyrrolidinyl]-2- oxoethyl]amino]-1-oxopropyl]-based DPP-IV inhibitors was synthesized. SAR studies resulted in a number of DPP-IV inhibitors, having IC50 values of 50 > 100 μM) and DPP-II (IC50 > 30 μM). Compound 21a suppressed the blood glucose elevation after an oral glucose challenge in Wistar rats and also inhibited plasma DPP-IV activity for up to 4 h in BALB/c mice. The results show that compound 21a possesses in vitro and in vivo activities comparable to those of NVP-LAF237 (4), which is in clinical development. 2006 American Chemical Society.

Pyrazolobenzamides and derivatives as factor Xa inhibitors

The present application describes pyrazolobenzamides and derivatives thereof of Formula I: [in-line-formulae]P4-P-M-M4??I [/in-line-formulae] or pharmaceutically acceptable salt forms thereof. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Orthogonally protected sugar diamino acids as building blocks for linear and branched oligosaccharide mimetics

It takes two: Sugar diamino acids which differ from established sugar amino acids by an additional amino group provide access to novel branched oligosaccharide mimetics and a novel class of aminoglycoside mimetics such as 1. The latter are of great signif

Synthesis of amides from unprotected amino acids by a simultaneous protection-activation strategy using dichlorodialkyl silanes

Reaction of L-phenylalanine (1) with dichlorodimethylsilane or other dichlorosilane derivatives 6b-d and primary amines leads to the formation of amides probably via a cyclic silyl intermediate. It is also possible to use β-amino acids and N-alkylated amino acids (peptoid building blocks) as well as the amino dicarboxylic acid L-aspartic acid. The latter leads to almost exclusive formation of the α-amide.

Synthesis and Biological Evaluation of Sparsomycin Analogues

Three series of sparsomycin analogues were prepared and examined for their ability to inhibit DNA or protein synthesis in bone marrow, P388 lymphocytic leukemia, and P815 mastocytoma cells.The compounds of series I and II, distinguished by the inclusion o