C07F9/301

A PROCESS FOR PREPARATION OF AN INTERMEDIATE OF L-GLUFOSINATE

The present invention provides a process for preparation of compound of formula (I), a key intermediate in synthesis of L-glufosinate or its salt. wherein P.sup.2 is an amino-protecting group; R.sup.1 is hydrogen, substituted or unsubstituted C.sub.1 to C.sub.6 alkyl group, a substituted or unsubstituted C.sub.1 to C.sub.6 alkenyl group, a substituted or unsubstituted C.sub.1 to C.sub.6 alkynyl group, a substituted or unsubstituted C.sub.3 to C.sub.10 cycloalkyl group, a substituted or unsubstituted C.sub.6 to C.sub.20 aryl group, or a substituted or unsubstituted C.sub.2 to C.sub.10 heteroaryl group; and X is a halogen or hydroxyl group.

A METHOD FOR OBTAINING L-GLUFOSINATE

The present invention relates to a safer, easier and cost-effective method for preparing L-glufosinate or salts thereof. The present invention further relates to a novel L-glufosinate quinine tetrahydrate salt and its use in a method for obtaining L-glufosinate or salts thereof.

METHODS FOR THE PURIFICATION OF L-GLUFOSINATE

Compositions and methods for isolating L-glufosinate from a composition comprising L-glufosinate and glutamate are provided. The method comprises converting the glutamate to pyroglutamate followed by the isolation of L-glufosinate from the pyroglutamate and other components of the composition to obtain substantially purified L-glufosinate. The composition comprising L-glufosinate and glutamate is subjected to an elevated temperature for a sufficient time to allow for the conversion of glutamate to pyroglutamate, followed by the isolation of L-glufosinate from the pyroglutamate and other components of the composition to obtain substantially purified L-glufosinate. The glutamate alternatively may be converted to pyroglutamate by enzymatic conversion. The purified L-glufosinate is present in a final composition at a concentration of 90% or greater of the sum of L-glufosinate, glutamate, and pyroglutamate. In some embodiments, a portion of the glutamate in the starting composition may be separated from the L-glufosinate using a crystallization step. Solid forms of L-glufosinate materials, including crystalline L-glufosinate ammonium, are also described.

Aminophosphinic derivatives that can be used in the treatment of pain

The present invention relates to a compound of the following general formula (I): R.sub.1NHCH(R.sub.2)P(O)(OR.sub.3)CH.sub.2C(R.sub.4)(R.sub.5)CONHCH(R.sub.6)COOR.sub.7 (I) or a pharmaceutically acceptable salt of the latter, an isomer or a mixture of isomers in any proportions, especially a mixture of enantiomers, and in particular a racemic mixture, for which R.sub.1 represents a C(O)OC(R.sup.8)(R.sup.9)OC(O)R.sup.10 group; R.sub.2 represents an optionally substituted hydrocarbon-based chain, an aryl or heteroaryl group or a methylene group substituted by a heterocycle; R.sub.3 represents a hydrogen atom or a C(R.sup.12)(R.sup.13)OC(O)R.sup.14 group; R.sub.4 and R.sub.5 form, together with the carbon that bears them, a saturated hydrocarbon-based ring or an optionally substituted piperidine ring or R.sub.4 represents a hydrogen atom and R.sub.5 represents a phenyl or a benzyl that is optionally substituted, a heteroaromatic ring or a methylene group substituted by a heterocycle; R.sub.6 represents an optionally substituted hydrocarbon-based chain or a phenyl or a benzyl that is optionally substituted; and R.sub.7 represents a hydrogen atom or a benzyl, alkyl, heteroaryl, alkylheteroaryl, CHMe-COOR.sup.18, CHR.sup.19OC(O)R.sup.20 and CHR.sup.19OC(O)OR.sup.20 group. The present invention also relates to the use of these compounds as a medicinal product, and in particular for the treatment of pain, more advantageously neuropathic and neuroinflammatory pain, to their method of synthesis and also to the compositions containing them.

Hydrophilic linkers and their uses for conjugation of drugs to a cell binding molecules
10131682 · 2018-11-20 · ·

Cell binding agent-drug conjugates comprising hydrophilic linkers, and methods of using such linkers and conjugates are provided.

HIGHLY STRETCHABLE, TRANSPARENT, AND CONDUCTIVE POLYMER

A polymer composition includes a conductive polymer and at least one stretchability and electrical conductivity (STEC) enhancer, wherein a content of the STEC enhancer in the composition is at least about 1 wt. % of the composition.

Method for preparing acrolein cyanohydrins
20180305303 · 2018-10-25 · ·

The present invention relates to an improved method for preparing acrolein cyanohydrins from hydrocyanic acid and the corresponding acroleins. The method is characterized in that the acrolein cyanohydrins obtained have a very low hydrocyanic acid content or are free of hydrocyanic acid and are therefore particularly well suited as intermediates for the synthesis of glufosinates.

SINGLE PHASE LIQUIDS OF ALKANOLAMINE SALTS OF DICAMBA

The invention is a herbicidal composition containing an alkanolamine salt of an dicamba capable of remaining as a single phase liquid over a period of at least 1 week and containing low amounts of water and high loadings of the salt. Such herbicidal compositions are capable of remaining liquid in the absence of high amounts of water, thereby enhancing their capacity to remain liquid over an extended period of time when exposed to environmental conditions to improve their effectiveness to transport the active salt through a leafy substrate and can reduce transportation costs by increasing the salt loading without compromising the stability of the composition.

Mixtures of dialkylphosphinic acids and alkylphosphinic acids, a process for preparation thereof and use thereof

The invention relates to mixtures of at least one dialkylphosphinic acid of the formula (I) ##STR00001##
in which R.sup.1, R.sup.2 are the same or different and are each independently C.sub.1-C.sub.18-alkyl, C.sub.2-C.sub.18-alkenyl, C.sub.6-C.sub.18-aryl, C.sub.7-C.sub.18-alkylaryl,
with at least one alkylphosphonic acid of the formula (II) ##STR00002##
in which R.sup.3 is C.sub.1-C.sub.18-alkyl, C.sub.2-C.sub.18-alkenyl, C.sub.6-C.sub.18-aryl or C.sub.7-C.sub.18-alkylaryl;
to a process for preparation thereof and to the use thereof.

BISMUTH PERFLUOROALKYLPHOSPHINATES AS LEWIS ACID CATALYSTS

The invention relates to bismuth perfluoroalkylphosphinates as Lewis acid catalysts, the compounds, and processes for the preparation thereof.


Ar.sub.xBi[OP(O)(R.sub.f).sub.2].sub.3-x(Ia),


Ar.sub.3Bi[OP(O)(R.sub.f).sub.2].sub.2(Ib).