C07D307/92

3-substituted carbonyl-naphtho[2,3-B]furane derivative or pharmaceutically acceptable salt thereof

The present invention provides a compound of the following Formula (1) or a pharmaceutically acceptable salt thereof: ##STR00001##
wherein X is an oxygen atom and the like; Y is CO, SO.sub.2 and the like; R.sup.1 is an optionally-substituted C.sub.1-6 alkyl group, an optionally-substituted C.sub.1-6 alkylcarbonyl group and the like; R.sup.2 is an optionally-substituted C.sub.1-6 alkyl group, an optionally-substituted C.sub.1-6 alkoxy group, an optionally-substituted amino group, an optionally-substituted 5- to 12-membered monocyclic or polycyclic saturated heterocyclic group and the like; R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are independently a hydrogen atom and the like which exhibits excellent effects in suppressing the proliferation and sphere-forming ability of cancer cells, and can be useful as an antitumor drug or cell growth inhibitor.

Method for the conversion of Abienol to Sclarediol
10633314 · 2020-04-28 · ·

A method of selective conversion of Abienol, represented by formula 1, to Sclareodiol, represented by formula 2 ##STR00001##
by ozonolysis and subsequent reduction. The ozonolysis is carried out at temperatures above 60 C., preferably in nonhalogenated solvents. R is selected from H, acetals, aminals, optionally substituted alkyl groups, such as benzyl group, carboxylates such as acetates or formates, carbonates such as methyl or ethyl carbonates, carbamates, and any protecting group which can be attached to 1 and cleaved from 2, R is selected from CHCH.sub.2, an alkyl moiety with C2-C20, e.g. CH.sub.2CH.sub.3, or a cycloalkyl or polycycloalkyl moiety with C3-C20, e.g. cyclopropyl, optionally alkylated, respectively, and the wavy bond is depicting an unspecified configuration of the adjacent double bond between C2 and C3.

Method for the conversion of Abienol to Sclarediol
10633314 · 2020-04-28 · ·

A method of selective conversion of Abienol, represented by formula 1, to Sclareodiol, represented by formula 2 ##STR00001##
by ozonolysis and subsequent reduction. The ozonolysis is carried out at temperatures above 60 C., preferably in nonhalogenated solvents. R is selected from H, acetals, aminals, optionally substituted alkyl groups, such as benzyl group, carboxylates such as acetates or formates, carbonates such as methyl or ethyl carbonates, carbamates, and any protecting group which can be attached to 1 and cleaved from 2, R is selected from CHCH.sub.2, an alkyl moiety with C2-C20, e.g. CH.sub.2CH.sub.3, or a cycloalkyl or polycycloalkyl moiety with C3-C20, e.g. cyclopropyl, optionally alkylated, respectively, and the wavy bond is depicting an unspecified configuration of the adjacent double bond between C2 and C3.

METHOD FOR THE PREPARATION OF (3E,7E)-HOMOFARNESIC ACID OR (3E,7E)-HOMOFARNESIC ACID ESTER

The invention provides an improved method of isolating the 3-(E)-isomer of an unsaturated carboxylic acid from a mixture of corresponding (E/Z)isomers. More particularly, the present invention relates to an improved method for the biocatalytic preparation of (3E,7E)-homofarnesylic acid; as well as a novel biocatalytic method for the improved preparation of homofarnesol, in particular of (3E,7E)-homofarnesol and homofarnesol preparations having an increased content of (3E,7E)-homofarnesol. The present invention also relates to methods of preparing()-ambroxby applying (3E,7E)-homofarnesylic acid or (3E,7E)-homofarnesol as obtained according to the invention as starting material.

Method for producing 2-acetyl-4H,9H-naphtho[2,3-B]furan-4,9-dione

The invention addresses the problem of providing a method for producing 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione that is suited to industrial production. The invention provides a method for producing 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione by reacting 3-bromo-3-buten-2-one and 2-hydroxy-1,4-naphthoquinone in the presence of a solvent, then obtaining crystals of 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione by adding an alcohol-based solvent and/or water to the reaction system, and treating the crystals by using a specific adsorbent in the presence of a solvent.

Method for producing 2-acetyl-4H,9H-naphtho[2,3-B]furan-4,9-dione

The invention addresses the problem of providing a method for producing 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione that is suited to industrial production. The invention provides a method for producing 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione by reacting 3-bromo-3-buten-2-one and 2-hydroxy-1,4-naphthoquinone in the presence of a solvent, then obtaining crystals of 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione by adding an alcohol-based solvent and/or water to the reaction system, and treating the crystals by using a specific adsorbent in the presence of a solvent.

4,9-DIOXO-4,9-DIHYDRONAPHTHO[2,3-B]FURAN-3-CARBOXAMIDE DERIVATIVES AND USES THEREOF FOR TREATING PROLIFERATIVE DISEASES AND INFECTIOUS DISEASES

The present disclosure provides compounds of Formulas (I), (II), and pharmaceutically acceptable salts thereof. The compounds described herein are useful in treating proliferative diseases, for example, cancer (e.g., lung cancer), and infectious diseases (e.g., bacterial infections).

##STR00001##

4,9-DIOXO-4,9-DIHYDRONAPHTHO[2,3-B]FURAN-3-CARBOXAMIDE DERIVATIVES AND USES THEREOF FOR TREATING PROLIFERATIVE DISEASES AND INFECTIOUS DISEASES

The present disclosure provides compounds of Formulas (I), (II), and pharmaceutically acceptable salts thereof. The compounds described herein are useful in treating proliferative diseases, for example, cancer (e.g., lung cancer), and infectious diseases (e.g., bacterial infections).

##STR00001##

General purpose plasticizers based on naphthalic acid diesters

A diester of a fused ring compound of the formula (I): ##STR00001##
wherein: the fused rings are both aromatic; R1 and R4 to R6 substituents are H or ester moieties having C1 to C20 linear or branched alkyl chains; R2 and R3 are C(O)OCxHy, wherein x is from 10 to 12 and y is from 21 to 25; two adjacent R1 to R4 substituents are C(O)OCxHy, wherein x is from 10 to 12 and y is from 21 to 25; and when R3 and R4 are ester moieties, the alkyl chains of R4 are not C5 or C8; and polymer compositions containing the fused ring compound.

PROCESS FOR THE PREPARATION OF UNSATURATED CARBOXYLIC ACIDS BY CARBONYLATION OF ALLYL ALCOHOLS AND THEIR ACYLATION PRODUCTS

The present invention relates to a process for carbonylating allyl alcohols at low temperature, low pressure and/or low catalyst loading. In an alternative embodiment, an acylation product of the allyl alcohol is used for the carbonylation. The present invention likewise relates to the preparation of conversion products of these carbonylation products and specifically of ()-ambrox.