Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.

Abstract: A process for and intermediates in the preparation of canfosfamide and its salts. Some of the intermediates have anticancer activity.

Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.

Abstract: Embodiments of the invention provide a method of using Schwartz Reagent, Cp2Zr(H)Cl, without accumulating or isolating it. Methods provide mixtures of Cp2ZrCl2, reductants that selectively reduce Cp2ZrCl2, and substrates. After reaction of Cp2ZrCl2 and the reductant, an intermediate reduction product is formed, apparently Schwartz Reagent. The in situ Schwartz Reagent then selectively reduces certain functional groups on the substrate. Substrates include tertiary amides, tertiary benzamides, aryl O-carbamates, and heteroaryl N-carbamates, which are reduced to aldehydes, benzaldehydes, aromatic alcohols, and heteroaromatics, respectively. Compared to prior methods, reagents are inexpensive and stable, reaction times are short, and reaction temperature in certain cases is conveniently room temperature. It has been estimated that using the in situ method described herein instead of synthesized or commercially obtained Schwartz Reagent provides a 50% reduction in cost.

Abstract: The invention provides a method for separating one or more triorganophosphite components from a crude phosphite mixture containing acidic hydrolysis products, the method comprising: contacting said crude phosphite mixture with a basic additive to produce a second mixture comprising a first phase and a second phase, wherein said first phase comprises the basic additive and one or more components independently selected from the group consisting of (R2O)(R3O)POH, (R1O)(HO)PO(H) and H3PO3, wherein R1, R2 and R3 are independently selected from the group consisting of C1 to C18 alkyl, C6 to C18 aryl and hydroxyaryl, and C3 to C18 cycloalkyl and hydroxyalkyl radicals, and wherein R2 and R3 can optionally be connected to each other directly by a chemical bond or through an intermediate divalent group R9; and said second phase comprises one or more triorganophosphite components independently selected from the group consisting of (R4O)(R5O)P(OR6) and ((R7O)(R8O)PO)nA, wherein R4, R5, R6, R7 and R8 are independently

Abstract: An improved process for the manufacture of formylphosphonic acid derivatives is reported. An aminomethylphosphonic acid substrate is contacted with a reagent selected from the group consisting of water, an alcohol, a phenol compound, and mixtures thereof and an oxidizing gas in the presence of a catalyst to form a reaction product mixture containing a formylphosphonic acid derivative and the conditions under which said contacting is carried out are controlled so that no more than 50% of the formylphosphonic acid derivative formed in the reaction product mixture is consumed by reaction with the reagent.

Abstract: The invention relates to a process for preparing N-phosphono-methylglycine by reacting a hexahydrotriazine compound with a triacyl phosphite in an organic solvent, hydrolyzing the resulting phosphono compound after prior extraction into an aqueous phase and separation from the organic phase. The process avoids decomposition of the organic solvent during hydrolysis.

Abstract: An improved process for the manufacture of formylphosphonic acid derivatives is reported. An aminomethylphosphonic acid substrate is contacted with a reagent selected from the group consisting of water, an alcohol, a phenol compound, and mixtures thereof and an oxidizing gas in the presence of a catalyst to form a reaction product mixture containing a formylphosphonic acid derivative and the conditions under which said contacting is carried out are controlled so that no more than 50% of the formylphosphonic acid derivative formed in the reaction product mixture is consumed by reaction with the reagent.

Abstract: An improved process for the manufacture of formylphosphonic acid derivatives is reported. An aminomethylphosphonic acid substrate is contacted with a reagent selected from the group consisting of water, an alcohol, a phenol compound, and mixtures thereof and an oxidizing gas in the presence of a catalyst to form a reaction product mixture containing a formylphosphonic acid derivative and the conditions under which said contacting is carried out are controlled so that no more than 50% of the formylphosphonic acid derivative formed in the reaction product mixture is consumed by reaction with the reagent.

Abstract: This invention relates to a new class of phosphoryl hydrazine compounds which are useful as insecticides, acaricides, anthelmintics, and nematocides, compositions containing the compounds, and methods for their use. This invention also relates to methods to produce such compounds.

Abstract: The present invention relates to an improved process for the preparation of an acyl derivative of O,S-dialkyl phosphoroamidothioate by reacting an O,S-dialkyl phosphoroamidothioate with an acylating agent in the presence of an acid, wherein the improvement resides in adding a C.sub.4 to C.sub.8 aliphatic alcohol, following completion of the acylation reaction, to the mixture of the N-acyl-O,S-dialkyl phosphoroamidothioate, the acylating agent and the acid. In an embodiment of the present invention, the acylation reaction is conducted in the absence of a solvent. The aliphatic alcohol is easily recovered and can be reused in a subsequent acylation reaction.

Abstract: Improved liquid phase process useful in the hydrocyanation of diolefinic compounds to produce nonconjugated acyclic nitriles and to the liquid phase process of isomerization of the nitriles to 3- and/or 4-monoalkene linear nitriles. The improvement involves conducting the process in the presence of zero-valent nickel and a multidentate phosphite ligand. The invention also provides a novel method of making phosphorochloridite.

Abstract: A process for the preparation of organophosphorus derivatives of 2,4-di-tert-butylphenol with a high proportion of organophosphorus derivatives of biphenyl, which comprises reacting, in a first step, a 4,4'-dihalobiphenyl whose halogen has an atomic weight of at least 35, under Grignard conditions with magnesium to form the corresponding Grignard compound and this is further reacted in a second step with bis(2,4-di-tert-butylphenyl) chlorophosphite with the formation of a mixture in which at least 50% by weight of the phosphorus is combined in the form of tetrakis(2,4-di-tert-butylphenyl) 4,4'-biphenylenediphosphonite. The invention further relates to a polyolefin molding composition containing tetrakis(2,4-di-tert-butylphenyl) 4,4'-biphenylenediphosphonite which was prepared by reaction of a 4,4'-dihalobiphenyl whose halogen has an atomic weight of at least 35 with magnesium to form the Grignard compound and by subsequent reaction with bis(2,4-di-tert-butylphenyl) chlorophosphite.

Abstract: An improved process for preparing a phosphorodichlorothioate of the formula ##STR1## wherein R is: a C.sub.1 -C.sub.10 alkyl group, optionally substituted with a C.sub.1 -C.sub.4 alkoxy group, a C.sub.1 -C.sub.4 Alkylthio group, or a halogen group; a C.sub.3 -C.sub.6 cycoalkyl group; a C.sub.7 -C.sub.10 araklyl group, optionally substituted with up to three C.sub.1 -C.sub.5 alkyl groups, C.sub.1 -C.sub.4 alkoxy groups, halogen groups or nitro groups, C.sub.6 -C.sub.10 aryl group, optionally substituted with up to three C.sub.3 -C.sub.5 alkyl groups, C.sub.1 -C.sub.4 alkoxy groups, halogen groups or nitro groups; which comprises reacting, at a temperature of from about -20.degree. C. to about 20.degree. C., a mercaptan of the formula R--SH, wherein R is as previously defined, with at least one chlorinating agent, sulfur based acid and phosphorus trichloride.

Abstract: A method of producing .alpha.-dihydropolyprenyl monophosphates from .alpha.-dihydropolyprenols through .alpha.-dihydropolyprenyl dichlorophosphates in good yield and with ease is provided. A method of producing .alpha.-dihydropolyprenyl dichlorophosphates which are intermediate compounds useful for the first-mentioned method is also provided.

Abstract: An optically active alpha-amino acid derivative having the formula: ##STR1## wherein: X is OH, Cl, Br, I, or OCOR.sub.3 ;Y is a radical selected to stabilize the alpha carbon atom of the alpha-amino acid derivative sufficiently to prevent significant change in symmetry thereof during replacement of X with an alkyl, aryl, alkenyl, alkynyl, alkaryl, aralkyl, alkenaryl or alkynaryl radical, or such radical having one or more chemical constituents thereon; andR.sub.1 and R.sub.2 are different from one another and are each hydrogen or an alkyl, aryl, alkenyl, alkynyl, alkaryl, aralkyl, alkenaryl, or alkynaryl radical, or such radical having one or more non-protic chemical constituents thereon is conventionally synthesized from the corresponding alpha-amino acid. The ##STR2## portion of the above derivative is converted to a ketone functionality without racemization.