C07D211/72

CONJUGATED DIYNES AND THEIR USE AS FLAVOR MODIFIERS
20230345986 · 2023-11-02 · ·

The present disclosure generally provides conjugates diynes, particularly 6,8-diyne amides, and the use of such compounds and related compounds as flavor modifiers. In some aspects, the disclosure provides compositions that include such conjugated diynes, such as compositions that include such conjugated diynes and one or more additional compounds, such as a sweetener, salt, a glutamate, an arginate, and the like. In some other aspects, the disclosure provides methods of reducing or eliminating the amount of sweetener, salt, glutamate, or arginate in a food or beverage product.

FUNGICIDAL ARYL AMIDINES

This disclosure relates to aryl amidines of Formula I and their use as fungicides.

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FUNGICIDAL ARYL AMIDINES

This disclosure relates to aryl amidines of Formula I and their use as fungicides.

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Compounds for inhibiting the activity of SARS-COV-2 spike glycoprotein
11034655 · 2021-06-15 ·

The present invention relates to compounds of formula (I) and its analogues (II) and (III): in which R.sub.1-R.sub.14, X, Y, Z.sub.1-Z.sub.4 are in the Summary of the Invention; capable of inhibiting the activity of RBD of SARS-COV-2 in its “closed” conformation before it binds with the human ACE2 receptor. The invention further provides a process for the preparation of compounds of the invention. ##STR00001##

Compounds for inhibiting the activity of SARS-COV-2 spike glycoprotein
11034655 · 2021-06-15 ·

The present invention relates to compounds of formula (I) and its analogues (II) and (III): in which R.sub.1-R.sub.14, X, Y, Z.sub.1-Z.sub.4 are in the Summary of the Invention; capable of inhibiting the activity of RBD of SARS-COV-2 in its “closed” conformation before it binds with the human ACE2 receptor. The invention further provides a process for the preparation of compounds of the invention. ##STR00001##

IL-6 INHIBITORS AND METHODS OF TREATMENT
20210206718 · 2021-07-08 ·

The instant invention describes compounds having IL-6 modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by IL-6.

Process for the preparation of (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine

The present disclosure is related to an improved and efficient process for preparation of (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine which comprises: (a) N-acylation of 3-Amino-4-methyl pyridine; (b) Quarternization of 3-Acetylamino-4-methyl pyridine using benzyl halide; (c) Partial reduction of quarternized 3-Acetylamino-4-methyl pyridine by Sodium borohydride in Methanol or water; (d) Hydrolysis of partially reduced product to 1-Benzyl-4-methylpiperidin-3-one in presence of acid; (e) Reductive amination of 1-Benzyl-4-methylpiperidin-3-one using Methanolic methylamine in presence of Titanium(IV) isopropoxide in Methanol; (f) Resolution of 1-Benzyl-4-methylpiperidin-3-yl)-methylamine using Ditoluoyl (L) tartaric acid to get (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine. The disclosure is also related to novel intermediates: ##STR00001##
wherein R, R and X are as described in the specification.

Process for the preparation of (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine

The present disclosure is related to an improved and efficient process for preparation of (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine which comprises: (a) N-acylation of 3-Amino-4-methyl pyridine; (b) Quarternization of 3-Acetylamino-4-methyl pyridine using benzyl halide; (c) Partial reduction of quarternized 3-Acetylamino-4-methyl pyridine by Sodium borohydride in Methanol or water; (d) Hydrolysis of partially reduced product to 1-Benzyl-4-methylpiperidin-3-one in presence of acid; (e) Reductive amination of 1-Benzyl-4-methylpiperidin-3-one using Methanolic methylamine in presence of Titanium(IV) isopropoxide in Methanol; (f) Resolution of 1-Benzyl-4-methylpiperidin-3-yl)-methylamine using Ditoluoyl (L) tartaric acid to get (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine. The disclosure is also related to novel intermediates: ##STR00001##
wherein R, R and X are as described in the specification.

Method for preparing 4-(piperidin-4-yl)morpholine

The object of the present invention is to provide a method for preparing 4-(piperidin-4-yl)morpholine, which is easy to operate. The object can be solved by a method for preparing 4-(1-benzylpiperidin-4-yl)morpholine, characterized in that 5-fold molar or more of morpholine is added to 1-benzyl-4-piperidone, and the mixture is reacted with hydrogen under 1 MPa or less in the presence of platinum catalyst or palladium catalyst.

UV absorbing compounds, compositions comprising same and uses thereof

There is provided a range of novel compounds which have been demonstrated to have useful electromagnetic radiation absorbing properties. These compounds will find use in a range of applications such as active components in sunscreen formulations, paints, plastics, fabrics, glass and UV protective coatings.