C07C2602/08

Inhibitors of alpha 2 beta 1 integrin and methods of use thereof

Disclosed herein, inter alia, are inhibitors of alpha 2 beta 1 integrin and methods of using the same.

Preparation method for S-indoxacarb

A catalyst and a method for preparing S-indoxacarb using the catalyst. The catalyst is prepared using 3-tert-butyl-5-(chloromethyl)salicylaldehyde and cyclohexanediamine as raw materials, where an original quinine catalyst such as cinchonine is replaced with the catalyst for application in the asymmetric synthesis of tert-butyl hydroperoxide and 5-chloro-2-methoxycarbonyl-1-indanone ester, greatly improving selection in the asymmetric synthesis process, with the S-enantiomer content increasing from 75% to over 98%, achieving the recycling of a high-efficiency chiral catalyst, and greatly reducing production costs. The synthesis process of the catalyst is simple and is favorable for industrialization, and lays good foundations for the production of high-quality indoxacarb.

PROCESS OF PREPARING 3-FLUORO-5(((1R,2AR)-3,3,4,4-TETRAFLUORO-1,2A-DIHYDROXY-2,2A,3,4-TETRAHYDRO-1H-CYCLOPENTA[CD]INDEN-7-YL)-OXY)BENZONITRILE
20230202970 · 2023-06-29 ·

Disclosed herein are processes for preparing certain intermediates useful in the synthesis of 3-fluoro-5-(((1S,2aR)-1,3,3,4,4-pentafluoro-2a-hydroxy-2,2a,3,4-tetrahydro-1H-cyclopenta[cd]inden-7-yl)oxy)benzonitrile or a pharmaceutically acceptable salt thereof.

High penetration drugs and their compositions thereof for treatment of Parkinson diseases
11685739 · 2023-06-27 · ·

One aspect of the invention provides a composition of novel high penetration compositions (HPC) or a high penetration prodrug (HPP) for treatment of Parkinson's disease. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

PROCESS FOR THE PREPARATION OF INDANAMINE DERIVATIVES AND NEW SYNTHESIS INTERMEDIATES

Subject-matter of the invention is a process for the preparation of a key intermediate in the synthesis of indacaterol. Subject-matter of the invention are also new synthesis intermediates. Formula (I):

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CIRCULAR ECONOMY METHODS OF PREPARING UNSATURATED COMPOUNDS

Methods of preparing unsaturated compounds or analogs through dehydrogenation of corresponding saturated compounds and/or hydrogenation of aromatic compounds are disclosed.

1,3-Di-oxo-indene derivative, pharmaceutically acceptable salt or optical isomer thereof, preparation method thereof, and pharmaceutical composition containing same as an antiviral, active ingredient

Disclosed are 1,3-Dioxoindene derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The 1,3-Dioxoindene derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, cold, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.

USE OF MAGNETIC MESOPOROUS POLY(IONIC LIQUID) INTERFACIAL CATALYST IN HYDROGENATION REACTION AND PREPARATION OF BIODIESEL
20230182122 · 2023-06-15 ·

The disclosure provides use of an efficient, recyclable, green and friendly catalyst to realize a method of hydrogenation of an unsaturated alkene, and a method for preparing biodiesel through the transesterification of soybean oil with ethanol. The method of hydrogenation of the unsaturated alkene comprises performing a hydrogenation reaction of an unsaturated alkene at ambient temperature and atmospheric pressure by using a CO.sub.2 and magnetic dual-responsive mesoporous poly(ionic liquid) as a catalyst I, and using n-hexane and water as a solvent, to obtain a corresponding saturated alkane. The method for preparing biodiesel through transesterification of soybean oil with ethanol comprises performing a transesterification reaction of soybean oil with ethanol at a temperature of 25-90° C. and atmospheric pressure by using a CO.sub.2 and magnetic dual-responsive mesoporous poly(ionic liquid) as a catalyst II, to obtain the biodiesel.

RAS-INHIBITING INDENYL ACETAMIDE COMPOUNDS, COMPOSITIONS, AND USES
20170342021 · 2017-11-30 ·

Disclosed are compounds, for example, compounds of formula (I), wherein R, R.sub.0 R.sub.1-R.sub.8, n, X, Y, Y.sup.1, and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition, for example, cancer.

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Process for the preparation of 2,2′-bis-indenyl biphenyl ligands and their metallocene complexes

The invention relates to a novel process for the preparation of 2,2′-bis indenyl biphenyl ligands of following formula (3): The invention also relates to metallocene complexes prepared using the novel process for the preparation of 2,2-bis indenyl biphenyl ligands. The invention also relates to novel intermediates used in the process for the preparation of 2,2′-bis indenyl biphenyl ligands. ##STR00001##