154161-05-4

Upstream product

• 1676-81-9 N-benzyloxycarbonyl-L-serine methyl ester 
• 18162-48-6 tert-butyldimethylsilyl chloride 
• 69739-34-0 t-butyldimethylsiyl triflate 
• 1145-80-8 N-(benzyloxycarbonyl)-L-serine 
• 98642-61-6 (2S)-2-amino-3-(tert-butyldimethylsilanyloxy)propionic acid methyl ester 
• 501-53-1 benzyl chloroformate 
• 2788-84-3 (S)-serine methyl ester 

Downstream Products

• 154161-01-0 [(2S)-1-(tert-butyl-dimethyl-silanyloxymethyl)-2-oxo-ethyl]-carbamic acid benzyl ester 
• 823235-76-3 (3S,5S,6S)-6-benzyloxycarbonylamino-3,5,7-tris-(tert-butyl-dimethyl-silanyloxy)-heptanoic acid methyl ester 
• 823235-88-7 methyl (3S,5S,6S)-6-(((benzyloxy)carbonyl)amino)-7-((tert-butyldimethylsilyl)oxy)-3,5-dihydroxyheptanoate 
• 823235-74-1 (5S,6S)-6-benzyloxycarbonylamino-7-(tert-butyl-dimethyl-silanyloxy)-5-hydroxy-3-oxo-heptanoic acid methyl ester 
• 359455-05-3 [(1S,2S)-1-(tert-butyl-dimethyl-silanyloxymethyl)-3-(2,2-dimethyl-6-oxo-6H-[1,3]dioxin-4-yl)-2-hydroxy-propyl]-carbamic acid benzyl ester 

Relevant academic research and scientific papers

CYCLOPENTAPYRROLE OREXIN RECEPTOR AGONISTS

The present invention is directed to cyclopentapyrrole, furopyrrole and azabicycloheptane compounds which are agonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.

CHROMENOPYRIDINE DERIVATIVES AS PHOSPHATIDYLINOSITOL PHOSPHATE KINASE INHIBITORS

The invention relates to inhibitors of PI5P4K inhibitors useful in the treatment of cancers, neurodegenerative diseases, inflammatory disorders, and metabolic diseases, having the Formula (I); where A1, A2, G, R1, R2, R3, R4, and W are described herein.

C-Functionalized chiral dioxocyclam and cyclam derivatives with 1,2,3-triazole units: Synthesis, complexation properties and crystal structures of copper(ii) complexes

New C-functionalized syn- and anti-dioxocyclam and cyclam derivatives with 1,2,3-triazole units attached to carbon atoms within the skeleton were designed as valuable bifunctional chelating agents for applications in nuclear medicine. These macrocyclic chelators were prepared via a multi-step sequence involving α- and β-amino acids, and their copper(ii) complexation properties were evaluated. A solution structure in which the triazoles are in axially coordinating positions was proposed for the [Cu(anti-27)]2+ complex. Promising results have been obtained regarding the complexation kinetics (1/2 = 3.21 d, 5 M HCl, 50°C).

SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF

Disclosed are compounds having enhanced potency in the modulation of NMD A receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.

NOVEL 2'/3'/5'-(R/S)-SERINYL FUNCTIONALIZED OLIGONUCLEOTIDES

The present invention provides novel chiral serinyl functionalized tethered oligonucleotides i.e. R/S serinyl functionalized tethered oligonucleotides and the process of preparation thereof. Specifically, the present invention provides a modified nucleosi

Synthesis and properties of 2′-O-[R- and S-(2-amino-3-methoxy)propyl] (R-AMP and S-AMP) nucleic acids

Substitution at 2′-position by either amino- or methoxy-pendant groups of the antisense oligonucleotides (AONs) is known to enhance their therapeutic value. A simple modification is described here in which we introduce both these groups in the form of ena

ORGANIC COMPOUNDS

The present invention relates to compounds of the formula; and their use in therapy.

Useful synthesis of the main dehydrohexapeptide segment of a macrocyclic antibiotic, berninamycin B

The useful synthesis of tetradehydrohexapeptide segment 2, which is the main skeleton of a macrocyclic antibiotic, berninamycin B, was first achieved. The skeleton 2 is constructed, in turn, of 2-[(Z)-1-amino-1-propenyl]-5-methyl-oxazole-4-carboxylic acid, α-dehydroalanine (ΔAla), L-Val, 2-[1-amino-1-ethenyl]-5-methyloxazole-4-carboxylic acid residues, besides L-Thr and ΔAla at the N- and C-termini, respectively.

A short and efficient synthesis of N-Cbz-galantinic acid under promoter control on enantioselective acyclic stereoselection based on chiral oxazaborolidinone-promoted aldol reactions

An effective 'promoter control' on enantioselective acyclic stereoselection based on chiral oxazaborolidinone-promoted asymmetric aldol reactions has been found in the case of chiral N-protected α-amino aldehydes. An enantioselective synthesis of the title compound has been efficiently accomplished by using a sequence of the aldol reaction. (C) 2000 Elsevier Science Ltd.

Synthesis of a series of stromelysin-selective thiadiazole urea matrix metalloproteinase inhibitors

The synthesis and enzyme inhibition data for a series of thiadiazole urea matrix metalloproteinase (MMP) inhibitors are described. A broad screening effort was utilized to identify several thiadiazoles which were weak inhibitors of stromelysin. Optimization of the thiadiazole leads to include an α-amino acid side chain with variable terminal amide substituents provided a series of ureas which were moderately effective stromelysin inhibitors, with K(i)'s between 0.3 and 1.0 μM. The most effective analogues utilized an L-phenylalanine as the amino acid component. In particular, unsubstituted 46 had a K(i) of 710 nM, while the p-fluoro analogue 52 displayed increased potency (100 nM). Stromelysin inhibition was further improved using a pentafluorophenylalanine substituent which resulted in 70, a 14 nM inhibitor. While gelatinase inhibition was generally poor, the use of 1-(2-pyridyl)piperazine as the amide component usually provided for enhanced activity, with 71 inhibiting gelatinase with a K(i) of 770 nM. The combination of this heterocycle with a p-fluorophenylalanine substituent provided the only analogue, 69, with collagenase activity (13 μM). The SAR for analogues described within this series can be rationalized through consideration of the X-ray structure recently attained for 70 complexed to stromelysin. Uniquely, this structure showed the inhibitor to be completely orientated on the left side of the enzyme cleft. These results suggest that thiadiazole urea heterocycles which incorporate a substituted phenylalanine can provide selective inhibitors of stromelysin. Careful selection of the amide substituent can also provide for analogues with modest gelatinase inhibition.