- Preparation method for indanone compound
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The invention especially relates to a preparation method for an indanone compound, belonging to the field of organic synthesis. The preparation method for the indanone compounds comprises the following steps: 1) subjecting a compound as shown in a formula I and a compound as shown in a formula II to a condensation reaction so as to prepare a compound as shown in a formula III; 2) subjecting the compound as shown in the formula III to hydrolysis in the presence of alkali so as to prepare a compound as shown in a formula IV; and 3) carrying out acylation and ring closure on the compound as shownin the formula IV so as to prepare the as shown in a formula V. Compared with the prior art, the preparation method for the indanone compound in the invention has the advantages of low raw material cost, simple operation, low production of waste water, waste gas and industrial residues, high yield and the like, and is more suitable for industrial production; and compared with various traditionalpreparation methods for the indanone compound, the preparation method of the invention has obvious advantages and shows good industrialization prospects.
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- METHODS AND COMPOSITIONS RELATED TO A RETINOID RECEPTOR-SELECTIVE PATHWAY
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Provided herein are methods and compositions related to a retinoid receptor-selective pathway. As described herein, this pathway can be targeted to manipulate a tumor microenvironment. For example, the methods and compositions described herein can be used to induce apoptosis in a cancer cell. Further, the compositions described herein, including Sulindac and analogs thereof, can be used to target this pathway for the treatment or prevention of cancer in human patients.
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- Synthesis and SAR study of modulators inhibiting tRXRα-dependent AKT activation
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RXRα represents an intriguing and unique target for pharmacologic interventions. We recently showed that Sulindac and a designed analog could bind to RXRα and modulate its biological activity, including inhibition of the interaction of an N-terminally truncated RXRα (tRXRα) with the p85α regulatory subunit of phosphatidylinositol-3-OH kinase (PI3K). Here we report the synthesis, testing and SAR of a series of novel analogs of Sulindac as potential modulators for inhibiting tRXRα-dependent AKT activation. A new compound 30 was identified to have improved biological activity.
- Wang, Zhi-Gang,Chen, Liqun,Chen, Jiebo,Zheng, Jian-Feng,Gao, Weiwei,Zeng, Zhiping,Zhou, Hu,Zhang, Xiao-Kun,Huang, Pei-Qiang,Su, Ying
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p. 632 - 648
(2013/05/09)
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- Synthesis of five- and six-membered benzocyclic ketones through intramolecular alkene hydroacylation catalyzed by Nickel(0)/N-Heterocyclic Carbenes
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Getting some closure: Mechanistic studies supported the participation of an oxanickelacycle complex in the hydroacylation step of the title reaction, which proceeds without decarbonylation even in the absence of well-known chelation assistance by heteroatoms. Copyright
- Hoshimoto, Yoichi,Hayashi, Yukari,Suzuki, Haruka,Ohashi, Masato,Ogoshi, Sensuke
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supporting information
p. 10812 - 10815
(2013/01/15)
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- PROCESS FOR THE PREPARATION OF 6-FLUORO-2-METHYL-1-INDANONE
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A process for the preparation of 6-fluoro-2-methyl-l-indanone which relates to a process of preferential cyclization of (3-fluorophenyl)-isopropenyl-ketone to obtain 6-fluoro-2-methyl- 1-indanone regioisomer with respect to 4-fluoro-2-methyl-l-indanone regioisomer, is described.
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Page/Page column 5-7
(2008/06/13)
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- Method for treating a patient with neoplasia using Iressa
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This invention provides a method for treating a patient with neoplasia by an adjuvant therapy that includes treatment with an inhibitor of human epidermal growth factor receptor tyrosine kinase and a cGMP-specific phosphodiesterase inhibitor.
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- Methods for treatment of scleroderma
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Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes and other such inhibitors are useful for the treatment of scleroderma.
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- Methods for treatment of lupus erythematosus
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Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes and other such inhibitors are useful for the treatment of lupus erythematosus.
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- Methods for treatment of multiple sclerosis
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Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes and other such inhibitors are useful for the treatment of multiple sclerosis.
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- Methods for treatment of renal cell carcinoma
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A method of treating renal cell carcinoma in a mammal with that disease comprising administering to the mammal a physiologically effective amount of an inhibitor of PDE10.
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- Methods for treatment of diseases where GSK 3-beta is desired, and methods to identify compounds usefule for that
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A method for selecting compounds for the treatment of diseases where GSK3β is desired includes assessing whether the compounds cause an increase in PKG activity in the tissue of interest.
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- Methods for treatment of rheumatoid arthritis
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Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes and other such inhibitors are useful for the treatment of rheumatoid arthritis.
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- Methods for treatment of cystic fibrosis
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Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes and other such inhibitors are useful for the treatment of cystic fibrosis.
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- Methods for treatment of type I diabetes
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Substituted condensation products of -benzyl-3-indenylacetamides with heterocyclic aldehydes and other such inhibitors are useful for the treatment of type I diabetes.
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- Method for treating patients with diabetic retinopathy by administering substituted sulfonyl indenyl acetic acids and alcohols
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Substituted indenyl sulfonyl acetic acids, esters and alcohols are useful in the treatment of diabetic retinopathy.
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- Method for treating patients with macular degeneration by administering substituted sulfonyl indenyl acetic acids and alcohols
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Substituted indenyl sulfonyl acetic acids, esters and alcohols are useful in the treatment of macular degeneration.
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- Method for treating patients with acne by administering a CGMP-specific PDE inhibitor
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Inhibitors of cGMP-specific PDE are useful in the treatment of acne.
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- Substituted condensation products of 1H-indenyl-hydroxyalkanes with aldehydes for neoplasia
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Substituted condensation products of 1H-indenylhydroxyalkanes with aldehydes are useful for inducing or promoting apoptosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in the arresting and treatment of neoplasia, including precancerous and cancerous lesions.
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- Method for treating patients with acne by administering substituted sulfonyl indenyl acetic acids, amides and alcohols
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Substituted indenyl sulfonyl acetic acids, amides, and alcohols are useful in the treatment of acne.
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- Substituted condensation products of N-benzyl-3-indenylacetamides heterocyclic aldehydes for neoplasia
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Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes are useful for inducing or promoting apotosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in the arresting and treatment of neoplasias, including precancerous and cancerous lesions.
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- Method for treating patients having precancerous lesions with substituted indene derivatives
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Substituted indene derivatives are useful for treating patients having precancerous lesions and for inhibiting the growth of neoplastic cells.
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- Substituted condensation products of n-benzyl-3-indenyl acetamides with heterocyclic aldehydes
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Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes are useful for inducing or promoting apotosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in the arresting and treatment of neoplasias, including precancerous and cancerous lesions.
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- Method for treating patients with psoriasis by administering substituted sulfonyl indenyl acetic acids, esters and alcohols
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Substituted indenyl sulfonyl acetic acids, esters and alcohols are useful in the treatment of psoriasis.
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- Method for treating patients with sarcoidosis by administering substituted sulfonyl indenyl acetic acids, esters and alcohols
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Substituted indenyl sulfonyl acetic acids, esters and alcohols are useful in the treatment of sarcoidosis.
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- Substituted methoxy benzylidene indenyl-acetic and propionic acids for treating patients with precancerous lesions
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Substituted methoxy benzylidene indenyl compounds are useful in the treatment of precancerous lesions and neoplasms.
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- Lactone compounds for treating patient with precancerous lesions
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Substituted lactone compounds are useful in the treatment of precancerous lesions and neoplasms.
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- Lactone compounds for treating patients with precancerous lesions
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Substituted lactone compounds are useful in the treatment of precancerous lesions.
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- Method for treating patients with precancerous lesions by administering substituted sulfonyl idenyl acetic and propionic acids and esters to patients with lesions sensitive to such compounds
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Substituted indenyl sulfonyl acetic acids are useful in the treatment of precancerous lesions sensitive to treatment with those sulfonyl compounds.
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- Esters and amides of substituted indenyl acetic acids
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Esters and amides of substituted indenyl acetic acids of the formula: n is an integer of at least 2;, Q is a deprotonated residue of polymer or macromolecular structure having a molecular weight of at least about 1000 containing at least two primary and/or secondary amino groups and/or hydroxy groups;, R1 is selected from hydrogen, lower alkyl, or haloalkyl;, R2 is selected from hydrogen or alkyl;, R3 and R4 are one or more members each independently chosen from hydrogen, alkyl, acyloxy, alkoxy, nitro, amino, acylamino, alkylamino, diakylamino, dialkylaminoalkyl, sulfamyl, alkythio, mercapto, hydroxy, hydroxyalkyl, alkylsulfonyl, halogen, cyano, carboxyl, carbalkoxy, carbamido, haloalkyl or cycloalkoxy; and, R5 is selected from alkylsulfenyl, alkylsulfinyl or alkylsulfonyl. are useful in the treatment of colonic polyps.
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