摘要:
The invention provides compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein [D] is the residue of a drug having a reactive functional group, said functional group being attached, directly or through a bridging group, via an oxygen-phosphorus bond to the phosphorus atom of the ##STR2## moiety; R.sub.1 is C.sub.1 -C.sub.8 alkyl, C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.12 aralkyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.4 -C.sub.9 heteroaryl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloheteroalkyl or C.sub.7 -C.sub.12 aralkyl; and R.sub.3 is selected from the group consisting of C.sub.1 -C.sub.8 alkyl; C.sub.2 -C.sub.8 alkenyl having one or two double bonds; (C.sub.3 -C.sub.7 cycloalkyl)-C.sub.r H.sub.2r -- wherein r is zero, one, two or three, the cycloalkyl portion being unsubstituted or bearing 1 or 2 C.sub.1 -C.sub.4 alkyl substituents on the ring portion; (C.sub.6 -C.sub.10 aryloxy)C.sub.1 -C.sub.8 alkyl; 2-, 3- or 4-pyridyl; and phenyl-C.sub.r H.sub.2r -- wherein r is zero, one, two or three and phenyl is unsubstituted, or is substituted by 1 to 3 alkyl each having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, halo, trifluoromethyl, dialkylamino having 2 to 8 carbon atoms or alkanoylamino having 2 to 6 carbon atoms. The compounds are adapted for targeted drug delivery, especially to the brain.
摘要:
Diazinon is prepared by coverting the starting hydroxypyrimidine to its potassium salt by reacting it with potassium carbonate in an organic solvent after removal of the water by azeotropic distillation, and reacting the resulting non-aqueous salt with diethyl thiophosphoryl chloride and recovering the diazinon formed, wherein the quantity of potassium carbonate used relative to the starting hydroxypyrimidine is less than molar and desirably of a ratio in the range of 0.55 to 0.75.
摘要:
Diazinon is prepared by converting the starting hydroxypyrimidine to its potassium salt by reacting it with potassium carbonate in an organic solvent after removal of the water by azeotropic distillation, and reacting the resulting non-aqueous salt with diethyl thiophosphoryl chloride and recovering the diazinon formed. The solvent used is either MIBK or an aliphatic hydrocarbon desirably containing 1-20% MEK.
摘要:
Insecticidal O-(6-methyl-2-alkyl-pyrimidin-4-yl) O-alkyl thionoalkanephosphonates of the formula ##STR1## in which R stands for methyl or ethyl,R.sup.1 stands for methyl or ethyl andR.sup.2 stands for isopropyl or tert-butyl.
摘要:
The process which comprises ##STR1## in which R represents hydrogen, alkoxy, alkylamino or dialkylamino or represents optionally substituted radicals from the series comprising alkyl, cycloalkyl and aryl,R.sup.1 represents optionally substituted radicals from the series comprising alkyl, alkoxy, alkylthio, mono- or dialkylamino and phenyl,R.sup.2 represents optionally substituted alkyl,R.sup.3 represents alkyl, alkoxy or aryl,X represents oxygen or sulphur, andY represents halogen or a grouping --OCOR.sup.3.The intermediates do not have to be isolated. Some are new compounds.
摘要翻译:其中R代表氢,烷氧基,烷基氨基或二烷基氨基,或代表从包含烷基,环烷基和芳基的系列中任选取代的基团的方法,其包含 R 1表示任选取代的烷基,R 3表示烷基,烷氧基或芳基,X表示氧或硫,Y表示卤素或分组 - 取代的烷基,烷氧基,烷硫基, OCOR3。 中间体不必孤立。 有些是新化合物。
摘要:
Disclosed are selected O-(2-trichloromethyl-4-pyrimidinyl)-O,O-dialkyl phosphorothionates and O-(2-trichloromethyl-4-pyrimidinyl)-O,O-dialkyl phosphoronates having the formula: ##STR1## wherein Y is an atom selected from the group consisting of sulfur and oxygen; R is a lower alkyl group having 1 to 4 carbon atoms; R.sup.1 is hydrogen, a lower alkyl group having 1 to 4 carbon atoms, halo or nitro; and R.sup.2 is a lower alkyl group having 1 to 4 carbon atoms or an amino group. These compounds have been found to exhibit insecticidal activity.
摘要:
O-alkyl-O-(2-cyclopropyl-6-substituted-methyl-pyrimidin-4-yl)-(thiono)(thiol) phosphoric (phosphonic) acid esters and ester-amides of the formula ##STR1## in which R is alkyl,R.sup.1 is alkyl, alkoxy, alkylthio, alkylamino or phenyl,R.sup.2 is alkoxy or alkylthio, andX is oxygen or sulphur,which possess arthropodicidal properties.
摘要:
Organophosphorus esters, useful in increasing the resistance of keratinous materials to attack by keratin-eating insects, have the general formula: ##STR1## wherein: X and Y are independently O or S;R.sub.1 is an alkyl, alkoxy, alkylamino, dialkylamino or alkylmercapto radical having 1 to 6 carbon atoms; an amino or aryl radical;R.sub.2 is an alkyl radical having 1 to 6 carbon atoms;R.sub.3 is a radical of the general formula:--J--(K--L).sub.n ( 2)wherein:J is an aliphatic radical, or radical containing an aromatic or heterocyclic ring;K is one of the following radicals: ##STR2## linked to J through the oxygen atom in the case of (3), (5) or (6), and through the nitrogen atom in the case of (4), and in which the carbonyl oxygen atom of (3), (4) or (5), or one or both carbonyl oxygen atoms of (6) may be replaced by sulphur; R.sub.4 is hydrogen, an aryl radical, or an alkyl radical of 1 to 6 carbon atoms;L is a halogenated alkyl or alkenyl radical; an alkyl radical (having 1 to 4 carbon atoms) or aryl radical substituted with a vinylsulphonyl group, vinylsulphonamido group or precursors thereof; or a heterocyclic radical containing 1 to 4 halogen atoms attached to carbon atoms adjacent to a nitrogen atom of the ring, the ring being linked directly to K or through an alkylene group having 1 to 4 carbon atoms;n is 1 to 3.