25112-95-2

Upstream product

• 5020-41-7 2-(3-methoxyphenyl)-ethanol 
• 98-59-9 p-toluenesulfonyl chloride 
• 1798-09-0 m-methoxyphenylacetic acid 
• 18927-05-4 methyl (3-methoxyphenyl)acetate 

Downstream Products

• 76803-74-2 ethyl 4-(m-methoxyphenyl)-2-methyl-2-(2'-propenyl)butyrate 
• 76803-76-4 ethyl 2-methyl-4-(m-methoxyphenyl)-2-vinylbutyrate 
• 83846-00-8 1-Methoxy-3-(3-vinyl-pent-4-enyl)-benzene 
• 73593-68-7 (+)-(1S,7aS)-1-tert-Butoxy-1,2,3,6,7,7a-hexahydro-4-<2-(3-methoxyphenyl)ethyl>-7a-methyl-5H-inden-5-on 
• 73004-96-3 1-(2-chloroethyl)-3-methoxybenzene 
• 534596-00-4 1-[2-(3-Methoxy-phenyl)-ethyl]-1H-indole-2-carboxylic acid ethyl ester 
• 428439-23-0 (1R,7aR)-1-(1,1-dimethylethoxy)-1,2,3,6,7,7a-hexahydro-4-[2-(3-methoxyphenyl)ethyl]-7a-methyl-5H-inden-5-one 
• 3736-22-9 ent-17β-estradiol 
• 952741-98-9 (8α,9β,13α,14β,17β)-3-methoxyestra-1,3,5(10)-trien-17-ol p-nitrobenzoate 
• 428439-30-9 (8α,13α,14β,17β)-3-methoxyestra-1,3,5(10),9(11)-tetraen-17-ol p-nitrobenzoate 
• 428439-26-3 (1R,3aR,4S,7aR)-1-(1,1-dimethylethoxy)octahydro-4-[2-(3-methoxyphenyl)ethyl]-7a-methyl-5H-inden-5-one 
• 428439-27-4 (1R,3aR,4R,7aR)-1-(1,1-dimethylethoxy)octahydro-4-[2-(3-methoxyphenyl)ethyl]-7a-methyl-5H-inden-5-one 
• 534596-02-6 1-[2-(3-Methoxy-phenyl)-ethyl]-1H-indole-2-carboxylic acid 
• 76803-91-3 2,3-dimethyl-2-phenethyl-3-cyclopenten-1-one 

Relevant academic research and scientific papers

Structure-Guided Development of Small-Molecule PRC2 Inhibitors Targeting EZH2-EED Interaction

Disruption of EZH2-embryonic ectoderm development (EED) protein-protein interaction (PPI) is a new promising cancer therapeutic strategy. We have previously reported the discovery of astemizole, a small-molecule inhibitor targeting the EZH2-EED PPI. Herein, we report the cocrystal structure of EED in complex with astemizole at 2.15 ?. The structure elucidates the detailed binding mode of astemizole to EED and provides a structure-guided design for the discovery of a novel EZH2-EED interaction inhibitor, DC-PRC2in-01, with an affinityKdof 4.56 μM. DC-PRC2in-01 destabilizes the PRC2 complex, thereby leading to the degradation of PRC2 core proteins and the decrease of global H3K27me3 levels in cancer cells. The proliferation of PRC2-driven lymphomas cells is effectively inhibited, and the cell cycle is arrested in the G0/G1 phase. Together, these data demonstrate that DC-PRC2in-01 could be an effective chemical probe for investigating the PRC2-related physiology and pathology and providing a promising chemical scaffold for further development.

Discovery, synthesis, and structure-activity relations of 3,4-dihydro-1H-spiro(naphthalene-2,2′-piperidin)-1-ones as potassium-competitive acid blockers

With the aim to discover a gastric antisecretory agent more potent than the existing proton pump inhibitors, novel 3,4-dihydro-1H-spiro(naphthalene-2,2′-piperidin)-1-one derivatives, which could occupy two important lipophilic pockets (described as LP-1 and LP-2) of H+,K+-ATPase and can strongly bind to the K+-binding site, were designed based on a docking model. Among the compounds synthesized, compound 4d showed a strong H+,K+-ATPase-inhibitory activity and a high stomach concentration in rats, resulting in potent inhibitory action on histamine-stimulated gastric acid secretion in rats. Furthermore, 4d exerted significant inhibitory action on histamine-stimulated gastric-acid secretion in rats with a rapid onset and moderate duration of action after the administration. These findings may lead to a new insight into the drug design of potassium-competitive acid blockers.

A facile total synthesis of ent-17β-estradiol and structurally related analogues

A facile six-step synthesis (15.2% yield) of ent-17β-estradiol from readily accessible precursors is described. The preparation of analogues with 2-alkyl substituents, double bond unsaturation in the C-ring, a cis C,D-ring fusion and modified substituents at C17 is also reported.

Opioid ligands with mixed properties from substituted enantiomeric N-phenethyl-5-phenylmorphans. Synthesis of a -agonist δ-antagonist and δ-inverse agonists

Enantiomeric N-phenethyl-m-hydroxyphenylmorphans with various substituents in the ortho, meta or para positions of the aromatic ring in the phenethylamine side-chain (chloro, hydroxy, methoxy, nitro, methyl), as well as a pyridylethyl and a indolylethyl m

New indole derivatives as factor Xa inhibitors

The present invention relates to compounds of formula I, in which R0; R1; R2; R3; R4; R5; R6; R7; Q; V, G and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is indicated. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as pharmaceuticals for treating the foregoing conditions, and pharmaceutical preparations comprising them.

The Structure and Function of Estrogens. XI. Synthesis of (+/-)-7(8->11α)abeo-Estradiol and its 9,11-Didehydro Derivative

Two approaches to the synthesis of (+/-)-7(8->11α)abeo-estra-1,3,5(10)triene-3,17β-diol (2a) from (+/-)-1β-t-butoxy-7aβ-methyl-2,3,3aα,6,7,7a-hexahydro-1H-inden-5(4H)-one (11) were studied.A pathway involving 6-alkylation of (11) with 2-(3'-methoxyphenyl)ethyl halides or sulfonate esters was unsuccessful, but conjugate addition of 3-methoxybenzyl nucleophiles with (+/-)-1β-t-butoxy-7aβ-methyl-6-methylene-2,3,3aα,6,7,7a-hexahydro-1H-inden-5(4H)-one (18), prepared from (11), led to (+/-)-1β-t-butoxy-6α--7aβ-methyl-2,3,3aα,6,7,7a-hexahydro-1H-inden-5(4H)-one (10a).Acid-catalyzed cyclization of (10a) afforded (+/-)-17β-t-butoxy-3-methoxy-7(8->11)abeo-estra-1,3,5(10),9(11)-tetraene (29) which upon lithium/ammonia reduction in the presence of diphenylmethane gave (+/-)-17β-t-butoxy-3-methoxy-7(8->11α)abeo-estra-1,3,5(10)-triene (31).Deprotection of (31) and (29) afforded (+/-)-7(8->11α)abeo-estra-1,3,5(10)-triene-3,17β-diol (2a) and (+/-)-7(8->11)abeo-estra-1,3,5(10),9(11)-tetraene-3,17β-diol (32), respectively. Alternatively, reaction of (+/-)-1β-t-butoxy-7aβ-methyl-6-methylene-2,3,3aα,6,7,7a-hexahydro-1H-inden-5(4H)-one (18) with 3-methoxybenzyl phenyl sulfoxide (23a) gave (1RS,3'SR,2RS,3a'SR,7a'SR)-3'-t-butoxy-2-(3''-methoxyphenyl)-3a'-methyl-2',3',3a',4',7',7a'-hexahydrospiroinden>-6'(1'H)-one (26), reductive cleavage of which with lithium/ammonia afforded (10a). The relative stereochemistries of (31) and of the spiro cyclopropyl ketone intermediate (26) were established unambiguously by X-ray crystallography.

Imidazo(4,5-C)pyridines as antiosteoporotic agents

This invention relates to 2-substituted-imidazo[4,5-c]pyridines, to the process for their preparation, to pharmaceutical compositions containing said 2-substituted-imidazo[4,5-c]pyridines and to the use of said 2-substituted-imidazo[4,5-c]pyridines for mo

A Stereoselective Approach to Steroid Trans C/D Ring Synthons

A stereoselective approach to the vitamin D skeleton that controls the stereochemistry at C13, C14, C17, and C20 is described.