177338-13-5

Upstream product

• 58479-61-1 tert-butylchlorodiphenylsilane 
• 627-18-9 1-bromo-3-propanol 

Downstream Products

• 221132-36-1 2-but-3-enyl-2-(3-tert-butyldiphenylsiloxy-propyl) malonic acid dimethyl ester 
• 203449-34-7 5-t-butyldiphenylsilanyloxy-2,2-dimethylpentanal 
• 358351-43-6 3-(3'-t-butyldiphenylsilyloxypropyl)cyclopentan-1-one 
• 777075-10-2 4-methyl-trans-4-hexenol tert-butyldiphenylsilyl ether 
• 405939-49-3 (6-amino-5-bromopyridin-3-yl)-[3-(tert-butyldiphenylsilanyloxy)propyl]carbamic acid benzyl ester 
• 626605-07-0 2-{1-[3-(tert-butyl-diphenyl-silanyloxy)-propyl]-1H-pyrrolo[2,3-b]pyridin-3-yl}-acetamide 
• 405939-50-6 (5-bromo-6-fluoropyridin-3-yl)-[3-(tert-butyldiphenylsilanyloxy)propyl]carbamic acid benzyl ester 
• 405939-80-2 (6-{5-[3-(tert-butyl-diphenyl-silanyloxy)-propylamino]-2-fluoro-pyridin-3-yl}-pyrazin-2-yl)-(3-chloro-phenyl)-carbamic acid tert-butyl ester 
• 405939-53-9 [6-(5-{benzyloxycarbonyl-[3-(tert-butyldiphenylsilanyloxy)propyl]amino}-2-fluoropyridin-3-yl)pyrazin-2-yl]-(3-chlorophenyl)carbamic acid tert-butyl ester 
• 405939-56-2 [6-(2-amino-5-{benzyloxycarbonyl-[3-(tert-butyldiphenylsilanyloxy)propyl]amino}pyridin-3-yl)pyrazin-2-yl]-(3-chloro-phenyl)carbamic acid tert-butyl ester 
• 1312750-65-4 1-benzyl-2-[5-((tert-butyl)diphenylsilanyloxy)pent-1-ynyl]-1-azaspiro[2.3]hexane 
• 1082207-46-2 5-((tert-butyldiphenylsilyl)oxy)-2-methyl-2-vinylpentanoic acid 
• 1361146-51-1 (S,Z)-6-((tert-butyldiphenylsilyl)oxy)hex-3-ene-1,2-diol 

Relevant academic research and scientific papers

TRIAZOLE FURAN COMPOUNDS AS AGONISTS OF THE APJ RECEPTOR

Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula (I) and Formula (II) have the following structures: (I); (II). Intermediates (V) are also claimed.

Novel pyrido[2,3-b]indole compounds for the treatment and prophylaxis of bacterial infection

The present invention relates to novel compounds of formula (I), wherein R1, R2, R3, R4, R5 and R6 are as described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.

BICYCLIC-PYRIMIDINEDIONE COMPOUNDS

The present invention provides novel bicyclic pyrimidinedione compounds that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions associated with left ventricular hypertrophy or diastolic dysfunction. The synthesis and characterization of the compounds is described, as well as methods for treating HCM and other forms of heart disease.

TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF

The present invention is directed to substituted indole compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, adisease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.

Asymmetric Synthesis of Spiroketals with Aminothiourea Catalysts

Chiral spiroketal skeletons are found as core structures in a range of bioactive compounds. These natural compounds and their analogues have attracted much attention in the field of drug discovery. However, methods for their enantioselective construction are limited, and easily available optically active spiroketals are rare. We demonstrate a novel catalytic asymmetric synthesis of spiroketal compounds that proceeds through an intramolecular hemiacetalization/oxy-Michael addition cascade mediated by a bifunctional aminothiourea catalyst. This results in spiroketal structures through the relay formation of contiguous oxacycles, in which multipoint recognition by the catalyst through hydrogen bonding imparts high enantioselectivity. This method offers facile access to spiroketal frameworks bearing an alkyl group at the 2-position, which are prevalent in insect pheromones. Optically active (2S,5S)-chalcogran, a pheromone of the six-spined spruce bark beetle, and an azide derivative could be readily synthesized from the bicyclic reaction product. Around and around: A catalytic asymmetric synthesis of spiroketals through an intramolecular hemiacetalization/oxy-Michael addition cascade with a bifunctional aminothiourea catalyst was developed. This method offers facile access to spiroketal frameworks bearing an alkyl group at the 2-position. Optically active (2S,5S)-chalcogran, a pheromone from the six-spined spruce bark beetle, and a derivative were readily synthesized from the bicyclic reaction product.

Total synthesis of (-)-zampanolide and structure-activity relationship studies on (-)-dactylolide derivatives

A new total synthesis of the marine macrolide (-)-zampanolide (1) and the structurally and stereochemically related non-natural levorotatory enantiomer of (+)-dactylolide (2), that is, ent-2, has been developed. The synthesis features a high-yielding, selective intramolecular Horner-Wadsworth-Emmons (HWE) reaction to close the 20-membered macrolactone ring of 1 and ent-2. The β-keto phosphonate/aldehyde precursor for the ring-closure reaction was obtained by esterification of a ω-diethylphosphono carboxylic acid fragment and a secondary alcohol fragment incorporating the THP ring that is embedded in the macrocyclic core structure of 1 and ent-2. THP ring formation was accomplished through a segment coupling Prins-type cyclization. Employing the same overall strategy, 13-desmethylene-ent-2 as well as the monocyclic desTHP derivatives of 1 and ent-2 were prepared. Synthetic 1 inhibited human cancer cell growth in vitro with nM IC50 values, while ent-2, which lacks the diene-containing hemiaminal-linked side chain of 1, is 25- to 260-fold less active. 13-Desmethylene-ent-2 as well as the reduced versions of ent-2 and 13-desmethylene-ent-2 all showed similar cellular activity as ent-2 itself. The same activity level was attained by the monocyclic desTHP derivative of 1. Oxidation of the aldehyde functionality of ent-2 gave a carboxylic acid that was converted into the corresponding N-hexyl amide. The latter showed only μM antiproliferative activity, thus being several hundred-fold less potent than 1. It's the side chain that matters: The marine macrolide (-)-zampanolide (1) has been synthesized via (-)-dactylolide (ent-2), the non-natural enantiomer of the marine natural product (+)-dactylolide (2), employing a high-yielding intramolecular Horner-Wadsworth-Emmons reaction to close the macrolactone ring. While the hemiaminal-linked side chain in 1 is crucial for nanomolar antiproliferative activity, the methylene group and the aldehyde functionality in ent-2 are dispensable. A monocyclic destetrahydropyran derivative of 1 shows equal activity as ent-2. Copyright

Total synthesis of resolvin E2

Resolvin E2 (2) was synthesized stereoselectively using the C1-8 and C15-20 aldehydes 6 and 9, which were connected to the C9-14 fragment by using Wittig reactions. The aldehyde 6 was prepared from the γ-silyl alcohol (S)-20 by a sequence of reactions involving ozonolysis, oxidation with NaIO4, and the Wittig reaction of the resulting aldehyde with Ph3P{double bond, long}CHCHO, whereas the aldehyde 9 was synthesized from the corresponding γ-silyl alcohol through epoxidation, reaction with Et2AlCN, and reduction with DIBAL-H.

Synthesis of precursors of phomactins using [2,3]-Wittig rearrangements

o-Toluic acid has been converted into methyl (8RS,9SR)-7-(bromomethyl)-8,9-dimethyl-1,4-dioxaspiro[4.5]dec-6-ene-8-carboxylate, the stereochemical defining step being a conjugate addition of lithium dimethylcuprate to a cyclohexadienone prepared using a B

Development of a new nonpeptidic self-immolative spacer. application to the design of protease sensing fluorogenic probes

The design and synthesis of novel self-immolative spacer systems aiming at the release of phenol-containing compounds are described. The newly designed traceless linkers proved to be conveniently stable under physiological conditions and operate through spontaneous decomposition of an hemithioaminal intermediate under neutral aqueous conditions. Their utility was then illustrated by the preparation of original fluorogenic substrates of penicillin amidase whose strong fluorescence is unveiled through enzyme-initiated domino reactions.

Hemisynthesis and preliminary evaluation of novel endocannabinoid analogues

Three new endocannabinoid analogues in which amide moiety was replaced either by oxomethylene group or ester moiety with simultaneous substitution of both α-hydrogens with methyl groups were synthesized and their abilities to interact with CB1-receptor and FAAH were investigated.