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Reformatsky reaction of 7-methoxyisochroman-4-one (Ia) and its sulphur analogue (Ib) with ethyl bromoacetate provides the hydroxy-esters (IIa) and (IIb) which on dehydration with fused KHSO4 afford the esters (IIIa) and (IIIb) respectively.Reduction of these esters with LAH yields the homoallylic alcohols (IVa) and (IVb) which on condensation with succinimide in the presence of diethyl azodicarboxylate and triphenylphosphine furnish the seco-steroids (Va) and (Vb) respectively.Reduction of these seco-steroids with NaBH4 at controlled pH results in the formation of ethoxyamides (VIa) and (VIb) which undergoe cyclisation in the presence of PTS to yield the title compounds (IXa,b).

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1,575-Naphthyridine – Wikipedia,
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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Safety of 2-(Dimethoxymethyl)-1,8-naphthyridine, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 204452-90-4, name is 2-(Dimethoxymethyl)-1,8-naphthyridine. In an article£¬Which mentioned a new discovery about 204452-90-4

Gold catalysis is a convenient tool to oxidatively functionalize alkyne into a range of valuable compounds. In this article, we report a new access to isochroman-4-one and 2H-pyran-3(6H)-one derivatives that involves a gold-catalyzed oxidative cycloalkoxylation of an alkyne in the presence of a pyridine N-oxide. The reaction proceeds under mild conditions, is relatively efficient and exhibits a high functional group compatibility.

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204452-90-4, Name is 2-(Dimethoxymethyl)-1,8-naphthyridine, belongs to naphthyridine compound, is a common compound. Computed Properties of C11H12N2O2In an article, once mentioned the new application about 204452-90-4.

A series of novel 4-isochromanone compounds bearing N-benzyl pyridinium moiety were designed and synthesized as acetylcholinesterase (AChE) inhibitors. The biological evaluation showed that most of the target compounds exhibited potent inhibitory activities against AChE. Among them, compound 1q possessed the strongest anti-AChE activity with an IC50 value of 0.15?nm and high AChE/BuChE selectivity (SI?>?5,000). Moreover, compound 1q had low toxicity in normal nerve cells and was relatively stable in rat plasma. Together, the current finding may provide a new approach for the discovery of novel anti-Alzheimer’s disease agents.

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The synthesis of compounds 6, 7a,b, 8a,b, 9a,b, and 10a,b where the amino -NH- group of JDTic (3) was replaced with an aromatic – CH-, CH2, O, S, or SO group was accomplished and used to further characterize the SAR of the compound 3 class of kappa opioid receptor antagonists. All of the compounds showed subnanomolar to low nanomolar Ke values at the kappa opioid receptor. The most potent compound was 7a, where the amino -NH- group of 3 was replaced by a methylene (-CH2-) group. This compound had a K e = 0.18 nM and was 37- and 248-fold selective for the kappa relative to the mu and delta opioid receptors, respectively. Similar to compound 3, compound 7a antagonized selective kappa agonist U50,488-induced diuresis after sc administration in rats. In contrast to 3, where kappa antagonist activity lasted for three weeks, compound 7a did not show any kappa antagonist activity after one week.

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XJP-L (8), a derivative of the natural product (¡À)-7,8-dihydroxy-3-methylisochroman-4-one isolated from the peel of Musa sapien tum L., was found to exhibit weak inhibitory activity of tubulin polymerization (IC50 = 10.6 muM) in our previous studies. Thus, a series of 4-arylisochromene derivatives were prepared by incorporating the trimethoxyphenyl moiety into 8, among which compound (¡À)-19b was identified as the most potent compound with IC50 values ranging from 10 to 25 nM against a panel of cancer cell lines. Further mechanism studies demonstrated that (¡À)-19b disrupted the intracellular microtubule network, caused G2/M phase arrest, induced cell apoptosis, and depolarized mitochondria of K562 cells. Moreover, (¡À)-19b exhibited potent in vitro antivascular and in vivo antitumor activities. Notably, the R-configured enantiomer of (¡À)-19b, which was prepared by chiral separation, was slightly more potent than (¡À)-19b and was much more potent than the S-configured enantiomer in both antiproliferative and antitubulin assays. Our findings suggest that (¡À)-19b deserves further research as a potential antitubulin agent for the treatment of cancers.

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1,573-Naphthyridine – Wikipedia,
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