Abstract: Phosphonium-based ionic conjugates (PBICs) are described. The PBICs each include a cationic binding partner comprising a phosphonium ion and an anionic binding partner comprising a pharmaceutically active compound, or prodrug, or derivative thereof. The conjugate can have at least one enhanced physiochemical, pharmacokinetic and/or therapeutic quality as compared to the pharmaceutically active compound when not provided in a PBIC. The phosphonium-containing cationic binding partner can also serve to enhance delivery of the anionic binding partner to the cytosol and/or the inner mitochondrial space. Methods of preparing the PBICs and using the PBICs to treat disease are also described.

Abstract: Phosphonium-based ionic conjugates (PBICs) are described. The PBICs each include a cationic binding partner comprising a phosphonium ion and an anionic binding partner comprising a pharmaceutically active compound, or prodrug, or derivative thereof. The conjugate can have at least one enhanced physiochemical, pharmacokinetic and/or therapeutic quality as compared to the pharmaceutically active compound when not provided in a PBIC. The phosphonium-containing cationic binding partner can also serve to enhance delivery of the anionic binding partner to the cytosol and/or the inner mitochondrial space. Methods of preparing the PBICs and using the PBICs to treat disease are also described.

Abstract: The invention pertains to a process for producing a compound of formula (11) wherein R7 and R8 are each independently selected from H, halogen, alkyl, aryl, or alkylaryl, R42 is H or a protective group, R43 is H or R3, wherein R3 is a protective group, by contacting a compound of formula (10) with an olefmation reagent, wherein compound of formula (10) comprises a counter acid X1 when R42?H and R43?H.

Abstract: Methods of synthesizing prostaglandins, prostaglandin analogs and their synthetic intermediates are described. The methods can comprise metal-catalyzed metathesis reactions. Also provided are synthetic intermediates that can be used in the synthesis of the prostaglandins and prostaglandin analogs.

Abstract: Methods of synthesizing prostaglandins, prostaglandin analogs and their synthetic intermediates are described. The methods can comprise metal-catalyzed metathesis reactions. Also provided are synthetic intermediates that can be used in the synthesis of the prostaglandins and prostaglandin analogs.

Abstract: The presently disclosed subject matter provides methods of preparing synthetic prostacyclin analogs, including Beraprost, either as racemic mixtures or as single stereoisomers. Also provided are novel synthetic intermediates for use in these methods.

Abstract: The presently disclosed subject matter provides methods of preparing synthetic prostacyclin analogues, including Beraprost, either as racemic mixtures or as single stereoisomers. Also provided are novel synthetic intermediates for use in these methods.

Abstract: The presently disclosed subject matter provides a method of synthesizing prostaglandins and prostaglandin analogs comprising the ring closing metathesis of compounds of Formula (I). Also provided are novel compounds of Formula (I) and Formula (II). In addition to their use as synthetic intermediates in the presently disclosed methods, compounds of Formula (II) can be used as prostaglandin and/or prostaglandin analog prodrugs.

Abstract: A method of preparing a N-acyl-N,N?,N?-alkylenediamine trialkanoic acid ester comprising contacting a cyclic amidine with an ester of a haloalkanoic acid is provided. In some embodiments, the method involves preparing a N-acyl-N,N?,N?-ethylenediamine trialkanoic acid ester by contacting a 2-alkyl imidazoline with the ester of haloalkanoic acid. In some embodiments, the N-acyl-N,N?,N?-alkylenediamine trialkanoic acid ester is a synthetic intermediate in the preparation of a N-acyl-N,N?,N?-alkylenediamine trialkanoic acid or a salt thereof. In some embodiments, the method provides novel N-acyl-N,N?,N?-alkylenediamine trialkanoic acids and/or esters, which can be used, for example, as chelating agents.

Abstract: The presently disclosed subject matter provides a method of synthesizing prostaglandins and prostaglandin analogs comprising the ring closing metathesis of compounds of Formula (I). Also provided are novel compounds of Formula (I) and Formula (II). In addition to their use as synthetic intermediates in the presently disclosed methods, compounds of Formula (II) can be used as prostaglandin and/or prostaglandin analog prodrugs.

Abstract: A method of preparing a N-acyl-N,N?,N?-alkylenediamine trialkanoic acid ester comprising contacting a cyclic amidine with an ester of a haloalkanoic acid is provided. In some embodiments, the method involves preparing a N-acyl-N,N?,N?-ethylenediamine trialkanoic acid ester by contacting a 2-alkyl imidazoline with the ester of haloalkanoic acid. In some embodiments, the N-acyl-N,N?,N?-alkylenediamine trialkanoic acid ester is a synthetic intermediate in the preparation of a N-acyl-N,N?,N?-alkylenediamine trialkanoic acid or a salt thereof. In some embodiments, the method provides novel N-acyl-N,N?,N?-alkylenediamine trialkanoic acids and/or esters, which can be used, for example, as chelating agents.

Abstract: The present invention provides novel quinazolinone compositions of matter comprising enantiomerically pure compound represented by Formula I: or a pharmaceutically acceptable salt thereof, having a detectable amount of one or more starting material and/or reagent used in the synthesis thereof.

Abstract: The present invention is directed to methods for the preparation of enantiomerically pure quinazolinones, intermediates in such methods, and compositions comprising such quinazolinones.

Abstract: The present invention provides intermediates, synthetic methods and novel quinazolinone compositions of matter.

Abstract: Disclosed are process steps and processes for producing chromane compounds, preferably 2-(6-amino-chroman-2yl) acetic acid esters which are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors.

Abstract: The present invention provides intermediates, synthetic methods and novel quinazolinone compositions of matter.

Abstract: A process for the preparation of 2-chloro-4,5-difluorobenzoic acid and 2,4,5-trifluorobenzoic acid as well as synthetic intermediates useful in and prepared according thereto, comprising reacting a nitrobenzene having the formula ##STR1## wherein X is chloro or fluoro, with an appropriate carbanion to form a compound having the formula ##STR2## wherein one of Y and Z is chloro and the other is nitro, and R is a radical selected from the group consisting of --CCl.sub.3, --CH.sub.2 NO.sub.2, --CH(NO.sub.2)R.sup.1, --CH(CO.sub.2 R.sup.1).sub.2, --CH(C(O)R.sup.2).sub.2, --CH(CN)CO.sub.2 R.sup.1, --CH(CO.sub.2 R.sup.1)COR.sup.2 and --COR.sup.2 where R.sup.1 is alkyl or arylalkyl and R.sup.2 is alkyl, aryl or arylalkyl and, where appearing more than once in such a radical, R.sup.1 and R.sup.2 may be the same or different at each occurrence.

Abstract: A process for the preparation of 2-chloro-4,5-difluorobenzoic acid and 2,4,5-trifluorobenzoic acid as well as synthetic intermediates useful in and prepared according thereto, comprising reacting a nitrobenzene having the formula ##STR1## wherein X is chloro or fluoro, with an appropriate carbanion to form a compound having the formula ##STR2## wherein one of Y and Z is chloro and the other is nitro, and R is a radical selected from the group consisting of --CCl.sub.3, --CH.sub.2 NO.sub.2, --CH(NO.sub.2)R.sup.1, --CH(CO.sub.2 R.sup.1).sub.2, --CH(C(O)R.sup.2).sub.2, --CH(CN)CO.sub.2 R.sup.1, --CH(CO.sub.2 R.sup.1)COR.sup.2 and --COR.sup.2 where R.sup.1 is alkyl or arylalkyl and R.sup.2 is alkyl, aryl or arylalkyl and, where appearing more than once in such a radical, R.sup.1 and R.sup.2 may be the same or different at each occurrence.

Abstract: A process for the preparation of 2-chloro-4,5-difluorobenzoic acid and 2,4,5-trifluorobenzoic acid as well as synthetic intermediates useful in and prepared according thereto, comprising reacting a nitrobenzene having the formula ##STR1## wherein X is chloro or fluoro, with an appropriate carbanion to form a compound having the formula ##STR2## wherein one of Y and Z is chloro and the other is nitro, and R is a radical selected from the group consisting of --CCl.sub.3, --CH.sub.2 NO.sub.2, --CH(NO.sub.2)R.sup.1, --CH(CO.sub.2 R.sup.1).sub.2, --CH(C(O)R.sup.2).sub.2, --CH(CN)CO.sub.2 R.sup.1, --CH(CO.sub.2 R.sup.1)COR.sup.2 and --COR.sup.2 where R.sup.1 is alkyl or arylalkyl and R.sup.2 is alkyl, aryl or arylalkyl and, where appearing more than once in such a radical, R.sup.1 and R.sup.2 may be the same or different at each occurrence.

Abstract: A process for the preparation of halobenzoic acids, comprising the step of reacting a halonitrobenzene with a pyridinium salt to form an intermediate of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl, aryl, alkenyl, alkynyl, --CN, --COOR' and --COR' where R' is alkyl or aryl; X is chloro or fluoro; Y is hydrogen, chloro or fluoro; and Z is chloro, bromo or iodo.