C07C45/64

Metal free process for allylic oxidation

The patent discloses a novel metal free process for the preparation of corresponding phenol and ketone via allylic oxidation of substituted cyclohexenes. Air is used as oxidant in the present process and can be used as such or optionally selected from pure oxygen or atmospheric oxygen. Moreover, the process of the present invention utilizes easily available starting materials and is a green eco-friendly, convenient and economical process with high yield of >60% and high selectivity.

METHOD FOR PREPARING A BENZOPHENONE DERIVATIVE
20220033580 · 2022-02-03 ·

The present invention is method comprising the steps of a) contacting 4-hydroxyphenone and a salt thereof with propylene oxide in a reactor heated to a temperature in the range of from 100° C. to 200° C. to form a poly(propylene oxide)-benzophenone intermediate; then b) contacting the intermediate with ethylene oxide in the heated reactor to form an alkoxylated benzophenone substituted with propylene oxide groups and ethylene oxide groups. The method of the present invention is useful for preparing a non-volatile alkoxylated benzophenone photoinitiator that gives long lasting gloss retention in an exterior architectural coating.

METHOD FOR PREPARING A BENZOPHENONE DERIVATIVE
20220033580 · 2022-02-03 ·

The present invention is method comprising the steps of a) contacting 4-hydroxyphenone and a salt thereof with propylene oxide in a reactor heated to a temperature in the range of from 100° C. to 200° C. to form a poly(propylene oxide)-benzophenone intermediate; then b) contacting the intermediate with ethylene oxide in the heated reactor to form an alkoxylated benzophenone substituted with propylene oxide groups and ethylene oxide groups. The method of the present invention is useful for preparing a non-volatile alkoxylated benzophenone photoinitiator that gives long lasting gloss retention in an exterior architectural coating.

METHOD FOR PREPARING A BENZOPHENONE DERIVATIVE
20220033580 · 2022-02-03 ·

The present invention is method comprising the steps of a) contacting 4-hydroxyphenone and a salt thereof with propylene oxide in a reactor heated to a temperature in the range of from 100° C. to 200° C. to form a poly(propylene oxide)-benzophenone intermediate; then b) contacting the intermediate with ethylene oxide in the heated reactor to form an alkoxylated benzophenone substituted with propylene oxide groups and ethylene oxide groups. The method of the present invention is useful for preparing a non-volatile alkoxylated benzophenone photoinitiator that gives long lasting gloss retention in an exterior architectural coating.

COMPOUND AND PREPARATION METHOD AND APPLICATION THEREOF
20210388007 · 2021-12-16 · ·

The present disclosure relates to a compound and a preparation method and application thereof, the compound having a chemical structure formula of:

##STR00001##

wherein M in the formula is selected from a group consisting of CF.sub.3 or CF.sub.2H, and R.sub.1, R.sub.2, and R.sub.3 are each independently selected from a group consisting of aryl, heteroaryl, and alkyl. The compound provided by the present disclosure can be used as a trifluoroethanolation reagent or difluoroethanolation reagent as synthetic intermediates of many organic compounds, and some of the compounds have pharmaceutical activity. The preparation steps of such compounds are simplified, with mild synthesis conditions and wide applicability of substrates.

COMPOUND AND PREPARATION METHOD AND APPLICATION THEREOF
20210388007 · 2021-12-16 · ·

The present disclosure relates to a compound and a preparation method and application thereof, the compound having a chemical structure formula of:

##STR00001##

wherein M in the formula is selected from a group consisting of CF.sub.3 or CF.sub.2H, and R.sub.1, R.sub.2, and R.sub.3 are each independently selected from a group consisting of aryl, heteroaryl, and alkyl. The compound provided by the present disclosure can be used as a trifluoroethanolation reagent or difluoroethanolation reagent as synthetic intermediates of many organic compounds, and some of the compounds have pharmaceutical activity. The preparation steps of such compounds are simplified, with mild synthesis conditions and wide applicability of substrates.

PROCESS FOR THE PRODUCTION OF SUBSTITUTED 2-[2-(PHENYL)ETHYLAMINO]ALKANEAMIDE DERIVATIVES

The present invention refers to a process for preparing a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R is (C.sub.3-C.sub.10)alkyl, or ω-trifluoro(C.sub.3-C.sub.10)alkyl; R.sub.1 and R.sub.2 are, independently, hydrogen, hydroxy, (C.sub.1-C.sub.8) alkoxy, (C.sub.1-C.sub.8) alkylthio, halo, trifluoromethyl or 2,2,2-trifluoroethyl; or one of R.sub.1 and R.sub.2 is in ortho position to the R—O— group and, taken together with the same R—O—, represents a Formula (A) group where R.sub.0 is (C.sub.2-C.sub.9)alkyl; R.sub.3 and R.sub.4 are, independently, hydrogen, (C.sub.1-C.sub.4)alkyl; or R.sub.4 is hydrogen and R.sub.5 is a group selected from —CH.sub.2—OH, —CH.sub.2—O—(C.sub.1-C.sub.6)alkyl, —CH(CH.sub.3)—OH, —(CH.sub.2).sub.2—S—CH.sub.3, benzyl and 4-hydroxybenzyl; or R.sub.4 and R.sub.5, taken together with the adjacent carbon atom, form a (C.sub.3-C.sub.6)cycloalkyl residue; R.sub.5 and R.sub.6 are independently hydrogen or (C.sub.1-C.sub.6)alkyl; or taken together with the adjacent nitrogen atom form a 5-6 membered monocyclic saturated heterocycle, optionally containing one additional heteroatom chosen among —O—, —S— and —NR.sub.7— where R.sub.7 is hydrogen or (C.sub.1-C.sub.6) alkyl; and wherein optionally one or more hydrogen atom in the groups R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6, preferably in the R group, can be substituted by a deuterium atom.

##STR00001##

PROCESS FOR THE PRODUCTION OF SUBSTITUTED 2-[2-(PHENYL)ETHYLAMINO]ALKANEAMIDE DERIVATIVES

The present invention refers to a process for preparing a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R is (C.sub.3-C.sub.10)alkyl, or ω-trifluoro(C.sub.3-C.sub.10)alkyl; R.sub.1 and R.sub.2 are, independently, hydrogen, hydroxy, (C.sub.1-C.sub.8) alkoxy, (C.sub.1-C.sub.8) alkylthio, halo, trifluoromethyl or 2,2,2-trifluoroethyl; or one of R.sub.1 and R.sub.2 is in ortho position to the R—O— group and, taken together with the same R—O—, represents a Formula (A) group where R.sub.0 is (C.sub.2-C.sub.9)alkyl; R.sub.3 and R.sub.4 are, independently, hydrogen, (C.sub.1-C.sub.4)alkyl; or R.sub.4 is hydrogen and R.sub.5 is a group selected from —CH.sub.2—OH, —CH.sub.2—O—(C.sub.1-C.sub.6)alkyl, —CH(CH.sub.3)—OH, —(CH.sub.2).sub.2—S—CH.sub.3, benzyl and 4-hydroxybenzyl; or R.sub.4 and R.sub.5, taken together with the adjacent carbon atom, form a (C.sub.3-C.sub.6)cycloalkyl residue; R.sub.5 and R.sub.6 are independently hydrogen or (C.sub.1-C.sub.6)alkyl; or taken together with the adjacent nitrogen atom form a 5-6 membered monocyclic saturated heterocycle, optionally containing one additional heteroatom chosen among —O—, —S— and —NR.sub.7— where R.sub.7 is hydrogen or (C.sub.1-C.sub.6) alkyl; and wherein optionally one or more hydrogen atom in the groups R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6, preferably in the R group, can be substituted by a deuterium atom.

##STR00001##

METHODS OF CARBON-CARBON BOND FRAGMENTATION
20220169580 · 2022-06-02 ·

The present disclosure relates to methods of carbon-carbon bond fragmentation.

METHODS OF CARBON-CARBON BOND FRAGMENTATION
20220169580 · 2022-06-02 ·

The present disclosure relates to methods of carbon-carbon bond fragmentation.