Patent classifications
C07D303/16
METHODS OF SYNTHESIZING A PROSTACYCLIN ANALOG
The present invention provides processes for preparing a prostacyclin analogue of Formula I
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R.sup.10 is a linear or branched C.sub.1-6 alkyl. The processes of the present invention comprise steps that generate improved yields and fewer byproducts than traditional methods. The processes of the present invention employ reagents (e.g., the oxidizing reagent) that are less toxic that those used in the traditional methods (e.g., oxalyl chloride). Many of the processes of the present invention generate intermediates with improved e.e. and chemical purity; thereby eliminating the need of additional chromatography steps. And, the processes of the present invention are scalable to generate commercial quantities of the final compound.
METHODS OF SYNTHESIZING A PROSTACYCLIN ANALOG
The present invention provides processes for preparing a prostacyclin analogue of Formula I
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R.sup.10 is a linear or branched C.sub.1-6 alkyl. The processes of the present invention comprise steps that generate improved yields and fewer byproducts than traditional methods. The processes of the present invention employ reagents (e.g., the oxidizing reagent) that are less toxic that those used in the traditional methods (e.g., oxalyl chloride). Many of the processes of the present invention generate intermediates with improved e.e. and chemical purity; thereby eliminating the need of additional chromatography steps. And, the processes of the present invention are scalable to generate commercial quantities of the final compound.
Green cationization agent
A compound having Formula (I) or Formula (II): ##STR00001## or a mixture thereof, in which R is H; CH.sub.3; CH(CH.sub.3).sub.2; CH.sub.2CH(CH.sub.3).sub.2; CH(CH.sub.3)CH.sub.2CH.sub.3; CH.sub.2(C.sub.6H.sub.5); CH.sub.2(3-indole); CH.sub.2CH.sub.2SCH.sub.3; CH.sub.2OH; CH(CH.sub.3)OH; CH.sub.2SH; CH.sub.2-(p-C.sub.6H.sub.4OH); CH.sub.2CH.sub.2CH.sub.2CH.sub.2NH.sub.2; CH.sub.2CONH.sub.2; CH.sub.2CH.sub.2CONH.sub.2; CH.sub.2CH.sub.2COOH; CH.sub.2COOH; or CH.sub.2CH.sub.2NHCNH.sub.2(NH.sub.2); and X is a suitable non-interfering anion, a process for making the compound having Formula (I) or Formula (II), and a process for reacting the compound having Formula (I) or Formula (II) or a mixture thereof with a (poly)saccharide to form a cationized (poly)saccharide.
Green cationization agent
A compound having Formula (I) or Formula (II): ##STR00001## or a mixture thereof, in which R is H; CH.sub.3; CH(CH.sub.3).sub.2; CH.sub.2CH(CH.sub.3).sub.2; CH(CH.sub.3)CH.sub.2CH.sub.3; CH.sub.2(C.sub.6H.sub.5); CH.sub.2(3-indole); CH.sub.2CH.sub.2SCH.sub.3; CH.sub.2OH; CH(CH.sub.3)OH; CH.sub.2SH; CH.sub.2-(p-C.sub.6H.sub.4OH); CH.sub.2CH.sub.2CH.sub.2CH.sub.2NH.sub.2; CH.sub.2CONH.sub.2; CH.sub.2CH.sub.2CONH.sub.2; CH.sub.2CH.sub.2COOH; CH.sub.2COOH; or CH.sub.2CH.sub.2NHCNH.sub.2(NH.sub.2); and X is a suitable non-interfering anion, a process for making the compound having Formula (I) or Formula (II), and a process for reacting the compound having Formula (I) or Formula (II) or a mixture thereof with a (poly)saccharide to form a cationized (poly)saccharide.
FUMAGILLOL TYPE COMPOUNDS AND METHODS OF MAKING AND USING SAME
The disclosure provides fumagillol type compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided.
FUMAGILLOL TYPE COMPOUNDS AND METHODS OF MAKING AND USING SAME
The disclosure provides fumagillol type compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided.
Preparation of vegetable oil-based monomers for use in thermosetting resins
The present embodiments herein generally relate to thermoset resins that are derived from vegetable oil based sources, including fibrous plant sources. The utilization of plant based oil as starting materials makes the technology a green alternative to currently available solutions. This, coupled with the novel synthetic methods that are utilized, results in a transformation of the plant based oils into useful, durable, and resilient thermoset resins.
Preparation of vegetable oil-based monomers for use in thermosetting resins
The present embodiments herein generally relate to thermoset resins that are derived from vegetable oil based sources, including fibrous plant sources. The utilization of plant based oil as starting materials makes the technology a green alternative to currently available solutions. This, coupled with the novel synthetic methods that are utilized, results in a transformation of the plant based oils into useful, durable, and resilient thermoset resins.
High-purity 3,4-epoxycyclohexylmethyl methacrylate
To provide 3,4-epoxycyclohexylmethyl methacrylate that is highly pure and that is useful as a raw material for functional materials or optical members having excellent transparency and heat resistance. An alicyclic epoxy compound product having a purity of 3,4-epoxycyclohexylmethyl methacrylate of 98.0 wt. % or greater and a total content of a compound represented by Formula (a) below and a compound represented by Formula (b) below of 1.3 wt. % or less. This alicyclic epoxy compound product preferably has a Hazen color number of 25 or less.
High-purity 3,4-epoxycyclohexylmethyl methacrylate
To provide 3,4-epoxycyclohexylmethyl methacrylate that is highly pure and that is useful as a raw material for functional materials or optical members having excellent transparency and heat resistance. An alicyclic epoxy compound product having a purity of 3,4-epoxycyclohexylmethyl methacrylate of 98.0 wt. % or greater and a total content of a compound represented by Formula (a) below and a compound represented by Formula (b) below of 1.3 wt. % or less. This alicyclic epoxy compound product preferably has a Hazen color number of 25 or less.