Patent classifications
C07C251/24
METHODS AND KITS FOR PREPARING RADIONUCLIDE COMPLEXES
A method for preparing a complex comprising a radioisotope of gallium for use in radiotherapy or in a medical imaging procedure, said method comprising adding a gallium radioisotope solution obtained directly from a gallium radionuclide generator to a composition comprising a pharmaceutically acceptable buffer and optionally also a pharmaceutically acceptable basic reagent, in amounts sufficient to increase the pH to a level in the range of 3 to 8, wherein the composition further comprises a chelator that is able to chelate radioactive gallium within said pH range and at moderate temperature, said chelator being optionally linked to a biological targeting agent. Kits and compositions for use in the method are also described and claimed.
Styryl carboxylate derivatives
Novel Styryl Carboxylate derivatives are provided which exhibit activity for the treatment of immunological diseases, inflammation, obesity, hyperlipidemia, hypertension, neurological diseases, and diabetes.
CLEAVABLE SURFACTANT
Cleavable surfactants of formula (I)
##STR00001##
having a total hydrophilic-lipophilic balance (HLB) of between 3 and 18 and wherein A is a group capable of releasing a flavor or fragrance aldehyde of formula (R.sup.1)CHO or a flavor or fragrance ketone of formula (R.sup.1)(R.sup.2)CO and is of formula
##STR00002##
wherein the wavy line indicates the location of the bond between L and A; R.sup.1 and R.sup.2 represent a hydrogen atom or a saturated or unsaturated C.sub.1-C.sub.18 hydrocarbon group, provided that at least one of the R.sup.1 or R.sup.2 groups has 6 consecutive carbon atoms and that both R.sup.1 and R.sup.2 taken together comprise a maximum of 18 carbon atoms; and L is a linear, branched or cyclic, saturated or unsaturated C.sub.3 to C.sub.40 hydrocarbon group. These surfactants solubilize and/or stabilize flavor and fragrance aldehydes and ketones in an aqueous environment and at the same time to control their release by hydrolysis.
METHOD OF PRODUCING PROTON PUMP INHIBITOR COMPOUND HAVING OPTICAL ACTIVITY
A highly pure optically active proton pump inhibitor compound can be produced safely and inexpensively in a high yield and enantioselectivity by a method of producing an optically active sulfoxide of Formula 2 or a salt thereof, comprising oxidizing a sulfide of Formula 1 or a salt thereof with hydrogen peroxide using an iron salt in the presence of a chiral ligand of Formula 3; wherein A is CH or N; R.sup.1 is hydrogen atom, an alkyl optionally substituted by halogen(s), or an alkoxy optionally substituted by halogen(s); one to three R.sup.2 may exist, and each of R.sup.2 is independently an alkyl, a dialkylamino, or an alkoxy optionally substituted by halogen(s) or alkoxy(s); each of R.sup.3 is independently hydrogen atom, a halogen, cyano or the like; R.sup.4 is a tertiary alkyl; and * and ** represent respectively R configuration or S configuration.
##STR00001##
METHOD OF PRODUCING PROTON PUMP INHIBITOR COMPOUND HAVING OPTICAL ACTIVITY
A highly pure optically active proton pump inhibitor compound can be produced safely and inexpensively in a high yield and enantioselectivity by a method of producing an optically active sulfoxide of Formula 2 or a salt thereof, comprising oxidizing a sulfide of Formula 1 or a salt thereof with hydrogen peroxide using an iron salt in the presence of a chiral ligand of Formula 3; wherein A is CH or N; R.sup.1 is hydrogen atom, an alkyl optionally substituted by halogen(s), or an alkoxy optionally substituted by halogen(s); one to three R.sup.2 may exist, and each of R.sup.2 is independently an alkyl, a dialkylamino, or an alkoxy optionally substituted by halogen(s) or alkoxy(s); each of R.sup.3 is independently hydrogen atom, a halogen, cyano or the like; R.sup.4 is a tertiary alkyl; and * and ** represent respectively R configuration or S configuration.
##STR00001##
Production method for 2-fluoro-4-borono-L-phenylalanine, and precursor of 2-fluoro-4-borono-L-phenylalanine
The present invention involves preparing compounds represented by the following formula: ##STR00001##
from a compound of the following formula: ##STR00002## In these formulae: R.sup.1 represents a Br group, an iodine group, a Cl group, an NO.sub.2 group, or an NH.sub.2 group; R.sup.2 represents a halogen group, an NO.sub.2 group, an NH.sub.2 group, Sn(R.sup.6).sub.3, NNNR.sup.7R.sup.8, OSO.sub.2R.sup.9, N R.sup.10R.sup.11, phenyliodonium, a heterocyclic group iodine, boric acid, or a borate ester; R.sup.30 represents a protective group PG.sup.1; R.sup.40 or R.sup.50 represent hydrogen, a protective group PG.sup.2, or C.sub.6H.sub.5(C.sub.6H.sub.5)CN, in which NR.sup.40R.sup.50 are together.
Production method for 2-fluoro-4-borono-L-phenylalanine, and precursor of 2-fluoro-4-borono-L-phenylalanine
The present invention involves preparing compounds represented by the following formula: ##STR00001##
from a compound of the following formula: ##STR00002## In these formulae: R.sup.1 represents a Br group, an iodine group, a Cl group, an NO.sub.2 group, or an NH.sub.2 group; R.sup.2 represents a halogen group, an NO.sub.2 group, an NH.sub.2 group, Sn(R.sup.6).sub.3, NNNR.sup.7R.sup.8, OSO.sub.2R.sup.9, N R.sup.10R.sup.11, phenyliodonium, a heterocyclic group iodine, boric acid, or a borate ester; R.sup.30 represents a protective group PG.sup.1; R.sup.40 or R.sup.50 represent hydrogen, a protective group PG.sup.2, or C.sub.6H.sub.5(C.sub.6H.sub.5)CN, in which NR.sup.40R.sup.50 are together.
Gossypol eflornithine Schiff base compound with antitumor activities and a method of preparing the same
A gossypol eflornithine Schiff base compound having the following Formula I: ##STR00001##
is disclosed. A method of preparing the compound of Formula I is also disclosed.
Gossypol eflornithine Schiff base compound with antitumor activities and a method of preparing the same
A gossypol eflornithine Schiff base compound having the following Formula I: ##STR00001##
is disclosed. A method of preparing the compound of Formula I is also disclosed.
Gossypol eflornithine Schiff base compound with antitumor activities and a method of preparing the same
A gossypol eflornithine Schiff base compound having the following Formula I: ##STR00001##
is disclosed. A method of preparing the compound of Formula I is also disclosed.