65298-99-9

Upstream product

• 108-24-7 acetic anhydride 
• 139-85-5 3,4-dihydroxybenzaldehyde 
• 65299-01-6 acetic acid 2-benzyloxy-5-formylphenyl ester 
• 67727-64-4 3,4-diacetoxybenzaldehyde 
• 75-36-5 acetyl chloride 

Downstream Products

• 134840-99-6 3-aetoxy-4-hydroxycinnamic acid 
• 110450-76-5 Acetic acid 2-[(E)-3-(3,4-dimethoxy-phenyl)-allyloxy]-5-formyl-phenyl ester 
• 881-57-2 isovanillin acetate 
• 65298-95-5 3-Acetoxy-4-(methoxymethoxy)benzaldehyd 
• 1147732-57-7 3-hydroxy-4-(spiro[4.5]dec-6-en-7-ylmethoxy)-benzaldehyde 
• 1147732-56-6 acetic acid 5-formyl-2-(spiro[4.5]dec-6-en-7-ylmethoxy)-phenyl ester (1.59 g). 
• 65299-01-6 acetic acid 2-benzyloxy-5-formylphenyl ester 
• 65299-00-5 3-hydroxy-4-(methoxymethoxy)benzaldehyde 
• 110450-68-5 4-[(E)-3-(3,4-Dimethoxy-phenyl)-allyloxy]-3-hydroxy-benzaldehyde 

Relevant academic research and scientific papers

Reinvestigation of acetylation of 3,4-dihydroxybenzaldehyde and reconciliation of previously reported analytical data

Acetylation of 3,4-dihydroxybenzaldehyde was reinvestigated. The results in the regiochemical outcome were analyzed in detail by NMR methods and compared with previously published data.

COMPOSITIONS AND METHODS FOR TREATING CANCER

The present disclosure relates to compounds that are capable penetrating to the blood brain barrier to modulate the activity of EGFR tyrosine kinase. The disclosure further relates to methods of treating Glioblastoma and other EGFR mediated cancers. The disclosure further relates to methods of treating Glioblastoma and other EGFR mediated cancers that have been determined to have altered glucose metabolism in the presence of inhibitors. The present disclosure also provides methods of administering to a subject a glucose metabolism inhibitor and a cytoplasmic p53 stabilizer.

IMMUNE CHECKPOINT INHIBITORS, COMPOSITIONS AND METHODS THEREOF

The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula (I), or a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof. For Formula (I) compounds R1, R2, X1, Y1 and n are as defined in the specification. The inventive Formula (I) compounds are inhibitors of the PD-1/PD-L1 protein/protein binding or functional interaction and find utility in any number of therapeutic applications, including but not limited to treatment of proliferative disorders such as cancer and infectious diseases.

CSJ acting as a versatile highly efficient greener resource for organic transformations

Simple, new, greener and efficient alternatives to the existing protocols have been developed for the reduction of aromatic aldehydes to their corresponding alcohols, decarboxylation of substituted benzoic acids (C6-C1) and substituted cinnamic acids (C6-C3) with a hydroxyl group at the para position with respect to the acid group to corresponding phenolic compounds and vinyl phenols respectively by using a natural feedstock, cucumber juice (CSJ), which acts as a greener solvent system, performing a substrate-selective reaction. Additionally, the hydrolysis of the acetyl as well as the benzoyl group of aromatic compounds has been carried out to afford excellent yield by CSJ.

Utilization of the inherent nucleophile for regioselective O-acylation of polyphenols via an intermolecular cooperative transesterification

A green and efficient method for regioselective O-acylation of polyphenols has been developed. The acylation can be carried out in potassium carbonate/dimethyl sulphoxide system by utilizing the ‘inherent nucleophile’ via an intermolecular cooperative transesterification under mild condition. This method shows particular advantage in regioselective acylation of polyphenols bearing 2′,4′-dihydroxyacetophenone moiety and can be extended to the synthesis of mono or multiple acetates of polyphenols without this moiety in good yields. Compared with other reported approaches, this method is endowed with atom economy and is more environment-friendly for avoiding the use of any metal-based catalysts.

PROCESS FOR PREPARING MORPHINE COMPOUNDS

The present application relates to processes for the preparation of morphine compounds utilizing a novel intramolecular [4+2] cycloaddition reaction.

Short chemoenzymatic total synthesis of ent-hydromorphone: An oxidative dearomatization/intramolecular [4+2] cycloaddition/amination sequence

A short synthesis of ent-hydromorphone has been achieved in twelve steps from β-bromoethylbenzene. The key transformations involved the enzymatic dihydroxylation of the arene to the corresponding cis-dihydrodiol, Mitsunobu coupling with the ring?A fragmen

PHARMACEUTICAL COMPOUNDS TARGETED BY MIF AFFINITY-TETHERED MOIETIES

There is disclosed a compound, a pharmaceutical composition and a method of treatment using a pharmaceutical composition comprising a tethering moiety that is capable of binding to a macrophage migration inhibitory factor (MIF) polypeptide, optionally linked to a linker moiety and further covalently bound to a drug moiety or imaging agent. More specifically, there is disclosed a genus of affinity-tethering moieties covalently bound to a drug moiety or imaging agent either directly or optionally via a linker moiety to covalently link the tethering moiety to a drug moiety. Without being bound by theory, the disclosed pharmaceutical compounds are targeted to cancer cells or immune cells via an affinity-tethering moiety that hitch-hikes to or into its target cell while bound to endogenous MIF.

First synthesis, characterization, and evidence for the presence of hydroxycinnamic acid sulfate and glucuronide conjugates in human biological fluids as a result of coffee consumption

A systematic investigation of the human metabolism of hydroxycinnamic acid conjugates was carried out. A set of 24 potential human metabolites of coffee polyphenols has been chemically prepared, and used as analytical standards for unequivocal identifications. These included glucuronide conjugates and sulfate esters of caffeic, ferulic, isoferulic, m-coumaric and p-coumaric acids as well as their dihydro derivatives. A particular focus has been made on caffeic and 3,4-dihydroxyphenylpropionic acid derivatives, especially the sulfate conjugates, for which regioselective preparation was particularly challenging, and have so far never been identified as human metabolites. Ten out of the 24 synthesized conjugates have been identified in human plasma and/or urine after coffee consumption. A number of these conjugates were synthesized, characterized and detected as hydroxycinnamic acid metabolites for the first time. This was the case of dihydroisoferulic acid 3′-O-glucuronide, caffeic acid 3′-sulfate, as well as the sulfate and glucuronide derivatives of 3,4-dihydroxyphenylpropionic acid.

SPIRO COMPOUNDS AND PHARMACEUTICAL USE THEREOF

The Spiro compound represented by the following general formula [Ia], its pharmaceutically acceptable salt or a solvate thereof