摘要:
The present invention is related to a new method for the synthesis of alpha-aminoalkylenephosphonic acid or its phosphonate esters comprising the steps of forming a reaction mixture by mixing a P-O-P anhydride moiety comprising compound, having one P-atom at the oxidation state (+111) and the other P-atom at the oxidation state (+111) or (+V), an aminoalkanecarboxylic acid and an acid catalyst, wherein said reaction mixture comprises an equivalent ratio of alpha-aminoalkylene carboxylic acid to P-O-P anhydride moieties of at least 0.2, and recovering the resulting alpha-aminoalkylene phosphonic acid compound or an ester thereof from the reaction mixture.
摘要:
A process for the catalyzed electrochemical reduction of carbon dioxide wherein a metal organic framework comprising metal ions and an organic ligand is used as a catalyst and novel metal organic frameworks based on bisphosphonic acids.
摘要:
The present invention provides novel compounds and ligands that are useful in transition metal catalyzed cross-coupling reactions. For example, the compounds and ligands of the present invention are useful in palladium or gold catalyzed cross-coupling reactions. The ligands are of formula (I) wherein each of R 1 and R 2 is independently selected from tert-butyl, cyclohexyl, 2-tolyl, or 1-adamantyl; each of R 3 and R 4 is independently selected from a C 1-5 alkyl, or R 3 , R 4 , and the nitrogen atom to which they are attached form an optionally substituted 4 -10 membered heterocyclic ring; each of X 1a and X 1b , is independently selected from N or C-R 5 ; each of X 2a and X 2b , is independently selected from N or C- R 6 ; each R 5 is independently selected from -H, -CH 3 , -OCH 3 , halogen, or -CF 3 ; each R 6 is independently selected from -H, -CH 3 , -OCH 3 , -N(CH 3 ) 2 , halogen, or -CF 3 ; or an R 5 and an R 6 located on adjacent carbon atoms together with the carbon atoms to which they are attached form an optionally substituted 5-7 membered heterocyclic or carbocyclic ring; or two R 6 groups together with the carbon atoms to which they are attached form an optionally substituted 5-7 membered heterocyclic or carbocyclic ring; and wherein no more than one of X 1a , X 1b , X 2a , or X 2b is N.
摘要:
Compounds of the following formula (I), for example: (1), wherein R , R , R , and R are described herein, are useful as inhibitors of plasma carboxypeptidase B. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.
摘要:
The invention relates to novel amidite derivatives and the use thereof as linker elements for synthesising polymers, especially biopolymers such as nucleic acids, peptides and saccharides, on the surface of solid carriers. The use of the inventive linker derivatives enables surfaces to be regenerated in a non-destructive manner.
摘要:
The invention concerns a ligand comprising wherein n is an integer from 1 to 5, X represents -NO2, -NH2, -NCS, -NHCOCH2-Z, NHCO-W-COCNHS, -NH-Q, -NHCS-Q, -NHCOCH2-Q, or -NHCO(CH2)m -Q where Q is an hapten chosen from the group consisting of steroids, enzymes, proteins, monoclonal antibodies, chimeric antibodies, or fragments thereof or any activated linker ready for coupling reaction, Y is CO2H or PO3H2 W is -(CH2)m- m is an integer from 1 to 10, Z is chloride, bromide or iodine.
摘要翻译:本发明涉及一种配体,其中n为1至5的整数,X表示-NO 2,-NH 2,-NCS,-NHCOCH 2 -Z,NHCO-W-COCNHS,-NH-Q,-NHCS-Q,-NHCOCH 2 -Q或-NHCO(CH 2)m -Q其中Q是选自类固醇,酶,蛋白质,单克隆抗体,嵌合抗体或其片段的半抗原或任何准备用于偶联反应的活化接头,Y是CO 2 H 或PO 3 H 2 W为 - (CH 2)m-m为1至10的整数,Z为氯,溴或碘。
摘要:
The invention discloses prodrugs comprising anti-proliferative drugs covalently linked, via a bridging group, to a phospholipid moiety such that the active species is preferentially released, preferably by enzymatic cleavage, at the required site of action. The invention further discloses pharmaceutical compositions comprising said prodrugs and the uses thereof for the treatment of diseases and disorders related to inflammatory, to degenerative or atrophic conditions, and to uncontrolled cell growth.
摘要:
The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds. Another aspect of the invention provides for the use of the chelation compounds described above in methods for diagnostic and therapeutic purposes. A diagnostic method is described for detecting the presence or absence of a target site within a mammalian host. This method comprises providing to cells a diagnostically effective dose of a compound of the present invention which contains a metal radionuclide, such as Tc and/or In, and detecting the biodistribution of the radionuclide. A therapeutic method is described for delivering a radionuclide, such as Re/ Re, Y, and Sm, to a target site within a mammalian host. This method comprises providing to cells a therapeutically effective dose of a chelate compound of the present invention.
摘要:
The present invention is directed to an improved process for preparing macrocyclic chelating agents and for conjugating the macrocyclic chelating agents to biological molecules.