C07C49/245

Gingerol derivative having inhibitory activity against biofilm formation and pharmaceutical composition comprising same as effective ingredient for preventing or treating biofilm-caused infection symptom

The present invention relates to a gingerol derivative having inhibitory activity against biofilm formation and a pharmaceutical composition for preventing or treating infections caused by biofilms including the gingerol derivative as an active ingredient. The gingerol derivative of the present invention exhibits significantly improved binding affinity for LasR and inhibitory activity against biofilm formation. Therefore, the gingerol derivative of the present invention can act on various membrane surfaces where biofilms tend to form and can effectively inhibit the formation of the corresponding biofilms. In addition, the use of the pharmaceutical composition according to the present invention can fundamentally prevent or treat a variety of infections caused by biofilms due to the presence of the gingerol derivative in the pharmaceutical composition.

Gingerol derivative having inhibitory activity against biofilm formation and pharmaceutical composition comprising same as effective ingredient for preventing or treating biofilm-caused infection symptom

The present invention relates to a gingerol derivative having inhibitory activity against biofilm formation and a pharmaceutical composition for preventing or treating infections caused by biofilms including the gingerol derivative as an active ingredient. The gingerol derivative of the present invention exhibits significantly improved binding affinity for LasR and inhibitory activity against biofilm formation. Therefore, the gingerol derivative of the present invention can act on various membrane surfaces where biofilms tend to form and can effectively inhibit the formation of the corresponding biofilms. In addition, the use of the pharmaceutical composition according to the present invention can fundamentally prevent or treat a variety of infections caused by biofilms due to the presence of the gingerol derivative in the pharmaceutical composition.

Functionalized cyanosilane and synthesis method and use thereof
10450331 · 2019-10-22 · ·

The present teachings relate to a functionalized silyl cyanide and synthetic methods thereof. As an example, the method may include adding a raw material silane and a cyanide source MCN in an organic solvent to produce the functionalized silyl cyanide in the absence of catalyst or in the presence of a metal salt catalyst. The functionalized silyl cyanide may be used in the reactions that classic TMSCN participates in, to synthesize important intermediates (e.g., cyanohydrin, amino alcohols and -amino nitrile compounds), with improved reactivity and selectivity. The cyanosilyl ether resulted from the nucleophilic addition of functionalized silyl cyanide to aldehyde or ketone may undergo intramolecular reaction under appropriate conditions to transfer the functional groups on silicon onto the other parts of the product linked to silicon. Such a functional group transfer process may increase the synthesis efficiency and atom economy, as well as afford products unobtainable using traditional TMSCN.

Functionalized cyanosilane and synthesis method and use thereof
10450331 · 2019-10-22 · ·

The present teachings relate to a functionalized silyl cyanide and synthetic methods thereof. As an example, the method may include adding a raw material silane and a cyanide source MCN in an organic solvent to produce the functionalized silyl cyanide in the absence of catalyst or in the presence of a metal salt catalyst. The functionalized silyl cyanide may be used in the reactions that classic TMSCN participates in, to synthesize important intermediates (e.g., cyanohydrin, amino alcohols and -amino nitrile compounds), with improved reactivity and selectivity. The cyanosilyl ether resulted from the nucleophilic addition of functionalized silyl cyanide to aldehyde or ketone may undergo intramolecular reaction under appropriate conditions to transfer the functional groups on silicon onto the other parts of the product linked to silicon. Such a functional group transfer process may increase the synthesis efficiency and atom economy, as well as afford products unobtainable using traditional TMSCN.

PRODUCTION OF FRAMBINONE BY A RECOMBINANT FUNGAL MICROORGANISM

The invention relates to a genetically modified fungal microorganism for the production of frambinone, said microorganism having the following characteristics: the capacity to produce frambinone from tyrosine; and a limited capacity or no capacity to break tyrosine down into tyrosol, p-hydroxyphenylacetaldehyde and/or p-hydroxyphenylacetate; and to the use of same for producing frambinone.

PRODUCTION OF FRAMBINONE BY A RECOMBINANT FUNGAL MICROORGANISM

The invention relates to a genetically modified fungal microorganism for the production of frambinone, said microorganism having the following characteristics: the capacity to produce frambinone from tyrosine; and a limited capacity or no capacity to break tyrosine down into tyrosol, p-hydroxyphenylacetaldehyde and/or p-hydroxyphenylacetate; and to the use of same for producing frambinone.

ARYL BETA DIKETONES AND THEIR USE AS ODORANTS
20190127305 · 2019-05-02 ·

The present invention refers to aryl beta diketones of the formula (I)

##STR00001## wherein Y, R.sup.1, R.sup.2 and R.sup.3 have the meaning R.sup.1 is selected from the group consisting of hydrogen, C.sub.1-C.sub.4 alkyl, hydroxyl, methoxy, CF.sub.3 and F; R.sup.2 is selected from the group consisting of methyl and ethyl; R.sup.3 is selected from the group consisting of methyl and ethyl; and Y is a bivalent residue selected from the group consisting of C(O); CH.sub.2CH.sub.2C(O); CR.sup.IR.sup.IIC(O), wherein R.sup.I and R.sup.II are independently selected from hydrogen and methyl; and CHR.sup.IIICHR.sup.IVC(O), wherein R.sup.III and R.sup.IV are independently selected from hydrogen and methyl with the proviso, that R.sup.IIIR.sup.IV are hydrogen or either R.sup.III or R.sup.IV is methyl. The invention further refers to fragrance compositions and fragranced articles comprising them.

SACUBITRIL INTERMEDIATE AND PREPARATION METHOD THEREOF

The present invention relates to a sacubitril intermediate and a preparation method thereof. The sacubitril intermediate disclosed herein can be prepared by a deprotection reaction of a compound. In addition, the intermediate can be used as a raw material to synthesize sacubitril. The method disclosed herein has advantages of easily obtained raw materials, simple preparation process, low cost, environment friendly, and etc., which is very suitable for industrial production.

Cyclobenzoins
10138192 · 2018-11-27 · ·

One-step cyanide-catalyzed benzoin condensations for synthesizing shape persistent cyclobenzoin macrocycles. Selected dialdehydes, and cyanide salts are reacted in aqueous solvents to form such cyclobenzoin macrocycles.

Cyclobenzoins
10138192 · 2018-11-27 · ·

One-step cyanide-catalyzed benzoin condensations for synthesizing shape persistent cyclobenzoin macrocycles. Selected dialdehydes, and cyanide salts are reacted in aqueous solvents to form such cyclobenzoin macrocycles.