869066-83-1Relevant articles and documents
Nitroxide derivative of ROCK kinase inhibitor
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Paragraph 0536-0542, (2020/06/17)
The invention provides a small molecular compound of a NO donor. The small molecular compound is characterized in that the small molecular compound is a compound shown represented by structural formula I shown in the description, or a stereoisomer, a geometrical isomer, a tautomer, a racemate, a deuterated isotope derivative, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof; and in the formula I, ring A is a substituted or unsubstituted heteroaromatic ring, X is selected from (CH2)n, n is selected from 0, 1, 2 and 3, R is a substituent group of terminal -O-NO2, R is selected from hydrogen, a hydroxyl group, halogen, an amino group, a cyano group, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group and a substituted or unsubstituted heteroalkyl group, and R and R are respectively and independently selected from hydrogen, a substituted or unsubstituted alkyl group, a substituted or unsubstituted naphthenic base or an amino protecting group, or R and R are connected to form a substituted or unsubstituted cyclic heteroalkyl group. The compound has a high-activity inhibition effect on ROCK kinase.
Synthesis method and application of 1-hydroxymethyl cyclopropyl acetic acid
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Paragraph 0026-0037, (2020/05/08)
The invention provides a synthetic method of 1-hydroxymethyl cyclopropyl acetic acid, which is an important intermediate of montelukast sodium serving as a raw material. The method comprises the following steps: by taking a compound bromomethyl cyclopropyl acetate as an initial raw material, preparing a Grignard reagent from the compound bromomethyl cyclopropyl acetate and magnesium strips or magnesium chips or magnesium powder under the initiation of an initiator; in the same reaction system, performing nucleophilic addition with dried carbon dioxide to prepare a compound, namely magnesium acetate bromide cyclopropyl ester; and carrying out ester hydrolysis on the magnesium bromide acetate cyclopropyl ester under an alkaline condition to obtain the 1-hydroxymethyl cyclopropyl acetic acid.The cost is effectively reduced; and synthesis steps are reduced, high-risk operation in the synthesis process is removed, safety risks are reduced, and environmental pollution is reduced.
SUBSTITUTED PIPERIDINES THAT INCREASE p53 ACTIVITY AND THE USES THEREOF
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Page/Page column 198, (2011/05/05)
The present invention provides a compound of Formula (1) as described herein or a pharmaceutically acceptable salt, solvate or ester thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
Process for making montelukast and intermediates therefor
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Page/Page column 10-11, (2008/06/13)
A process for making montelukast, a pharmaceutically useful compound of the following formula and salts thereof: using a compound of formula (20) is provided.