The present invention relates to a process for the one-pot hydrogenation and dehydration or isomerization of an organic compound, and to a catalyst composition for this process comprising transition metal particles having particle size below 50 nm supported on a material comprising at least one fluorinated polymer (P), wherein polymer (P) bears —SO.sub.2X functional groups, X being selected from X′ and OM, X′ being selected from the groups consisting of F, Cl, Br and I; and M being selected from the group consisting of H, and alkaline metal and NH.sub.4.

The present invention relates to a process for the one-pot hydrogenation and dehydration or isomerization of an organic compound, and to a catalyst composition for this process comprising transition metal particles having particle size below 50 nm supported on a material comprising at least one fluorinated polymer (P), wherein polymer (P) bears —SO.sub.2X functional groups, X being selected from X′ and OM, X′ being selected from the groups consisting of F, Cl, Br and I; and M being selected from the group consisting of H, and alkaline metal and NH.sub.4.

A reactor for performing a gas/liquid biphasic high-pressure reaction with a foaming medium, comprising an interior formed by a cylindrical, vertically oriented elongate shell, a bottom and a cap, wherein the interior is divided by internals into a backmixed zone and a zone of limited backmixing, wherein the backmixed zone and the zone of limited backmixing are consecutively traversable by the reaction mixture, wherein the backmixed zone comprises means for introducing gas and liquid and a gas outlet and also comprises at least one mixing apparatus selected from a stirrer, a jet nozzle and means for injecting the gas, and the zone of limited backmixing comprises a reaction product outlet, a first cylindrical internal element which in the interior extends in the longitudinal direction of the reactor and which delimits the zone of limited backmixing from the backmixed zone, backmixing-preventing second internal elements in the form of random packings, structured packings or liquid-permeable trays arranged in the zone of limited backmixing and a riser tube whose lower end is arranged within the backmixed zone and whose upper end opens into the zone of limited backmixing so that liquid from the backmixed zone can ascend into the zone of limited backmixing via the riser tube, wherein flow into the zone of limited backmixing enters from below. The reactor is configured such that the high-pressure reaction space is optimally utilized and contamination of workup steps or subsequent reactions arranged downstream of the high-pressure reaction with foam is substantially avoided. The invention further relates to a process for performing a continuous gas/liquid biphasic high-pressure reaction in the reactor.

A reactor for performing a gas/liquid biphasic high-pressure reaction with a foaming medium, comprising an interior formed by a cylindrical, vertically oriented elongate shell, a bottom and a cap, wherein the interior is divided by internals into a backmixed zone and a zone of limited backmixing, wherein the backmixed zone and the zone of limited backmixing are consecutively traversable by the reaction mixture, wherein the backmixed zone comprises means for introducing gas and liquid and a gas outlet and also comprises at least one mixing apparatus selected from a stirrer, a jet nozzle and means for injecting the gas, and the zone of limited backmixing comprises a reaction product outlet, a first cylindrical internal element which in the interior extends in the longitudinal direction of the reactor and which delimits the zone of limited backmixing from the backmixed zone, backmixing-preventing second internal elements in the form of random packings, structured packings or liquid-permeable trays arranged in the zone of limited backmixing and a riser tube whose lower end is arranged within the backmixed zone and whose upper end opens into the zone of limited backmixing so that liquid from the backmixed zone can ascend into the zone of limited backmixing via the riser tube, wherein flow into the zone of limited backmixing enters from below. The reactor is configured such that the high-pressure reaction space is optimally utilized and contamination of workup steps or subsequent reactions arranged downstream of the high-pressure reaction with foam is substantially avoided. The invention further relates to a process for performing a continuous gas/liquid biphasic high-pressure reaction in the reactor.

The present invention relates to a process for the preparation of an optically active carbonyl compound by asymmetric hydrogenation of a prochiral α,β-unsaturated carbonyl compound with hydrogen in the presence of at least one optically active transition metal catalyst that is soluble in the reaction mixture and which has rhodium as catalytically active transition metal and a chiral, bidentate bisphosphine ligand, wherein the reaction mixture during the hydrogenation of the prochiral α,β-unsaturated carbonyl compound additionally comprises at least one compound of the general formula (I): ##STR00001## in which R.sup.1, R.sup.2: are identical or different and are C.sub.6- to C.sub.10-aryl which is unsubstituted or carries one or more, e.g. 1, 2, 3, 4 or 5, substituents which are selected from C.sub.1- to C.sub.6-alkyl, C.sub.3- to C.sub.6-cycloalkyl, C.sub.6- to C.sub.10-aryl, C.sub.1- to C.sub.6-alkoxy and amino; Z is a group CHR.sup.3R.sup.4 or aryl which is unsubstituted or carries one or more, e.g. 1, 2, 3, 4 or 5, substituents which are selected from C.sub.1- to C.sub.6-alkyl, C.sub.3- to C.sub.6-cycloalkyl, C.sub.6- to C.sub.10-aryl, C.sub.1- to C.sub.6-alkoxy and amino, wherein R.sup.3 and R.sup.4 are as defined in the claims and the description.

The present invention relates to a process for the preparation of an optically active carbonyl compound by asymmetric hydrogenation of a prochiral α,β-unsaturated carbonyl compound with hydrogen in the presence of at least one optically active transition metal catalyst that is soluble in the reaction mixture and which has rhodium as catalytically active transition metal and a chiral, bidentate bisphosphine ligand, wherein the reaction mixture during the hydrogenation of the prochiral α,β-unsaturated carbonyl compound additionally comprises at least one compound of the general formula (I): ##STR00001## in which R.sup.1, R.sup.2: are identical or different and are C.sub.6- to C.sub.10-aryl which is unsubstituted or carries one or more, e.g. 1, 2, 3, 4 or 5, substituents which are selected from C.sub.1- to C.sub.6-alkyl, C.sub.3- to C.sub.6-cycloalkyl, C.sub.6- to C.sub.10-aryl, C.sub.1- to C.sub.6-alkoxy and amino; Z is a group CHR.sup.3R.sup.4 or aryl which is unsubstituted or carries one or more, e.g. 1, 2, 3, 4 or 5, substituents which are selected from C.sub.1- to C.sub.6-alkyl, C.sub.3- to C.sub.6-cycloalkyl, C.sub.6- to C.sub.10-aryl, C.sub.1- to C.sub.6-alkoxy and amino, wherein R.sup.3 and R.sup.4 are as defined in the claims and the description.

A reactor for performing a reaction between two immiscible fluids of different density, comprising an interior formed by a cylindrical, vertically oriented elongate shell, a bottom and a cap, wherein the interior is divided by internals into a backmixed zone, a zone of limited backmixing preferably arranged below the backmixed zone and a plug-flow zone which are at least consecutively traversable by one of the fluids, wherein the backmixed zone comprises at least one inlet and the plug-flow zone comprises an outlet and the backmixed zone comprises at least one mixing apparatus selected from a stirrer, a jet nozzle and means for injecting the fluid of lower density, a first cylindrical internal element which in the interior extends in the longitudinal direction of the reactor, which delimits the zone of limited backmixing from the plug-flow zone and which comprises a first passage to the backmixed zone and a second passage to the plug-flow zone, a second internal element which delimits the backmixed zone from the plug-flow zone such that there is no direct fluid connection between the backmixed zone and the plug-flow zone, and backmixing-preventing third internal elements in the form of random packings, structured packings or liquid-permeable trays arranged in the zone of limited backmixing. The reactor allows an optimal residence time distribution in the reaction of the two immiscible fluids of different density. The invention further relates to a process for performing a continuous reaction in the reactor.

A reactor for performing a reaction between two immiscible fluids of different density, comprising an interior formed by a cylindrical, vertically oriented elongate shell, a bottom and a cap, wherein the interior is divided by internals into a backmixed zone, a zone of limited backmixing preferably arranged below the backmixed zone and a plug-flow zone which are at least consecutively traversable by one of the fluids, wherein the backmixed zone comprises at least one inlet and the plug-flow zone comprises an outlet and the backmixed zone comprises at least one mixing apparatus selected from a stirrer, a jet nozzle and means for injecting the fluid of lower density, a first cylindrical internal element which in the interior extends in the longitudinal direction of the reactor, which delimits the zone of limited backmixing from the plug-flow zone and which comprises a first passage to the backmixed zone and a second passage to the plug-flow zone, a second internal element which delimits the backmixed zone from the plug-flow zone such that there is no direct fluid connection between the backmixed zone and the plug-flow zone, and backmixing-preventing third internal elements in the form of random packings, structured packings or liquid-permeable trays arranged in the zone of limited backmixing. The reactor allows an optimal residence time distribution in the reaction of the two immiscible fluids of different density. The invention further relates to a process for performing a continuous reaction in the reactor.

This invention relates to cocrystals of naloxone and of naltrexone and their use as opioid antagonists. The cocrystals of the invention include naloxone isonicotinamide cocrystal, naloxone hydrochloride piperazine cocrystal, naltrexone menthol cocrystal, naltrexone thymine cocrystal, naltrexone 2,5-dihydroxybenzoic acid cocrystal, naltrexone salicylic acid cocrystal, naltrexone hydrochloride piperazine cocrystal and naltrexone hydrochloride sulfathiazole cocrystal. A drug-in¬ adhesive transdermal patch containing the opioid analgesic fentanyl or an analog thereof and a cocrystal of naloxone or naltrexone is disclosed. Also disclosed is a method of treating pain, such as acute, chronic or intermittent pain, by applying a drug-in-adhesive transdermal patch of the invention to the skin of a patient in need thereof. Also disclosed is an improved transdermal patch for administering fentanyl or an analog thereof, or for administering a mu opioid agonist, the improvement wherein the transdermal patch contains a cocrystal of the invention in an abuse limiting amount. The improved transdermal patch may be a drug-in-adhesive transdermal patch or a reservoir transdermal patch.

This invention relates to cocrystals of naloxone and of naltrexone and their use as opioid antagonists. The cocrystals of the invention include naloxone isonicotinamide cocrystal, naloxone hydrochloride piperazine cocrystal, naltrexone menthol cocrystal, naltrexone thymine cocrystal, naltrexone 2,5-dihydroxybenzoic acid cocrystal, naltrexone salicylic acid cocrystal, naltrexone hydrochloride piperazine cocrystal and naltrexone hydrochloride sulfathiazole cocrystal. A drug-in¬ adhesive transdermal patch containing the opioid analgesic fentanyl or an analog thereof and a cocrystal of naloxone or naltrexone is disclosed. Also disclosed is a method of treating pain, such as acute, chronic or intermittent pain, by applying a drug-in-adhesive transdermal patch of the invention to the skin of a patient in need thereof. Also disclosed is an improved transdermal patch for administering fentanyl or an analog thereof, or for administering a mu opioid agonist, the improvement wherein the transdermal patch contains a cocrystal of the invention in an abuse limiting amount. The improved transdermal patch may be a drug-in-adhesive transdermal patch or a reservoir transdermal patch.