Patent classifications
C07F9/72
Chemical synthesis of the organoarsenical antibiotic arsinothricin
The subject invention provides methods for the chemical synthesis of racemic arsinothricin (D,L-AST), the novel organoarsenical antibiotic. One is by condensation of the 2-chloroethyl(methyl)arsinic acid with acetamidomalonate, and the second involves reduction of the N-acetyl-protected derivative of hydroxyarsinothricin (AST-OH) and subsequent methylation of the resulting sodium salt of trivalent arsenic intermediate with methyl iodide. The enzyme AST N-acetyltransferase (ArsNl) was utilized to purify L-AST from racemic AST. This expedient chemical synthesis of AST provides a source of this novel antibiotic for future drug development.
Chemical synthesis of the organoarsenical antibiotic arsinothricin
The subject invention provides methods for the chemical synthesis of racemic arsinothricin (D,L-AST), the novel organoarsenical antibiotic. One is by condensation of the 2-chloroethyl(methyl)arsinic acid with acetamidomalonate, and the second involves reduction of the N-acetyl-protected derivative of hydroxyarsinothricin (AST-OH) and subsequent methylation of the resulting sodium salt of trivalent arsenic intermediate with methyl iodide. The enzyme AST N-acetyltransferase (ArsNl) was utilized to purify L-AST from racemic AST. This expedient chemical synthesis of AST provides a source of this novel antibiotic for future drug development.
CHEMICAL SYNTHESIS OF THE ORGANOARSENICAL ANTIBIOTIC ARSINOTHRICIN
The subject invention provides methods for the chemical synthesis of racemic arsinothricin (D,L-AST), the novel organoarsenical antibiotic. One is by condensation of the 2-chloroethyl(methyl)arsinic acid with acetamidomalonate, and the second involves reduction of the N-acetyl-protected derivative of hydroxyarsinothricin (AST-OH) and subsequent methylation of the resulting sodium salt of trivalent arsenic intermediate with methyl iodide. The enzyme AST N-acetyltransferase (ArsN1) was utilized to purify L-AST from racemic AST. This expedient chemical synthesis of AST provides a source of this novel antibiotic for future drug development.
CHEMICAL SYNTHESIS OF THE ORGANOARSENICAL ANTIBIOTIC ARSINOTHRICIN
The subject invention provides methods for the chemical synthesis of racemic arsinothricin (D,L-AST), the novel organoarsenical antibiotic. One is by condensation of the 2-chloroethyl(methyl)arsinic acid with acetamidomalonate, and the second involves reduction of the N-acetyl-protected derivative of hydroxyarsinothricin (AST-OH) and subsequent methylation of the resulting sodium salt of trivalent arsenic intermediate with methyl iodide. The enzyme AST N-acetyltransferase (ArsN1) was utilized to purify L-AST from racemic AST. This expedient chemical synthesis of AST provides a source of this novel antibiotic for future drug development.
Chemical synthesis of the organoarsenical antibiotic arsinothricin
The subject invention provides methods for the chemical synthesis of racemic arsinothricin (D,L-AST), the novel organoarsenical antibiotic. One is by condensation of the 2-chloroethyl(methyl)arsinic acid with acetamidomalonate, and the second involves reduction of the N-acetyl-protected derivative of hydroxyarsinothricin (AST-OH) and subsequent methylation of the resulting sodium salt of trivalent arsenic intermediate with methyl iodide. The enzyme AST N-acetyltransferase (ArsN1) was utilized to purify L-AST from racemic AST. This expedient chemical synthesis of AST provides a source of this novel antibiotic for future drug development.
Chemical synthesis of the organoarsenical antibiotic arsinothricin
The subject invention provides methods for the chemical synthesis of racemic arsinothricin (D,L-AST), the novel organoarsenical antibiotic. One is by condensation of the 2-chloroethyl(methyl)arsinic acid with acetamidomalonate, and the second involves reduction of the N-acetyl-protected derivative of hydroxyarsinothricin (AST-OH) and subsequent methylation of the resulting sodium salt of trivalent arsenic intermediate with methyl iodide. The enzyme AST N-acetyltransferase (ArsN1) was utilized to purify L-AST from racemic AST. This expedient chemical synthesis of AST provides a source of this novel antibiotic for future drug development.
USE OF AT LEAST ONE BINARY GROUP 15 ELEMENT COMPOUND, A 13/15 SEMICONDUCTOR LAYER AND BINARY GROUP 15 ELEMENT COMPOUNDS
The invention provides the use of at least one binary group 15 element compound of the general formula R.sup.1R.sup.2E-E′R.sup.3R.sup.4 (I) or R.sup.5E(E′R.sup.6R.sup.7)2 (II) as the educt in a vapor deposition process. In this case, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently selected from the group consisting of H, an alkyl radical (C1-C10) and an aryl group, and E and E′ are independently selected from the group consisting of N, P, As, Sb and Bi. This use excludes hydrazine and its derivatives. The binary group 15 element compounds according to the invention allow the realization of a reproducible production and/or deposition of multinary, homogeneous and ultrapure 13/15 semiconductors of a defined combination at relatively low process temperatures. This makes it possible to completely waive the use of an organically substituted nitrogen compound such as 1.1 dimethyl hydrazine as the nitrogen source, which drastically reduces nitrogen contaminations—compared to the 13/15 semiconductors and/or 13/15 semiconductor layers produced with the known production methods.
USE OF AT LEAST ONE BINARY GROUP 15 ELEMENT COMPOUND, A 13/15 SEMICONDUCTOR LAYER AND BINARY GROUP 15 ELEMENT COMPOUNDS
The invention provides the use of at least one binary group 15 element compound of the general formula R.sup.1R.sup.2E-E′R.sup.3R.sup.4 (I) or R.sup.5E(E′R.sup.6R.sup.7)2 (II) as the educt in a vapor deposition process. In this case, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently selected from the group consisting of H, an alkyl radical (C1-C10) and an aryl group, and E and E′ are independently selected from the group consisting of N, P, As, Sb and Bi. This use excludes hydrazine and its derivatives. The binary group 15 element compounds according to the invention allow the realization of a reproducible production and/or deposition of multinary, homogeneous and ultrapure 13/15 semiconductors of a defined combination at relatively low process temperatures. This makes it possible to completely waive the use of an organically substituted nitrogen compound such as 1.1 dimethyl hydrazine as the nitrogen source, which drastically reduces nitrogen contaminations—compared to the 13/15 semiconductors and/or 13/15 semiconductor layers produced with the known production methods.
Synthesis of the organoarsenical antibiotic arsinothricin and derivatives thereof
The subject invention provides methods and procedures for synthesis and/or semi-synthesis of the novel antibiotic arsinothricin (AST) and derivatives. Arsinothricin (AST), a new broad-spectrum organoarsenical antibiotic, is a non-proteinogenic analog of glutamate that effectively inhibits glutamine synthetase. The subject invention provides chemical synthesis of an intermediate in the pathway of AST synthesis, hydroxyarsinothricin (AST-OH), which can be converted to AST by enzymatic methylation catalyzed by the ArsM As(III) S-adenosylmethionine methyltransferase. The methods provide a source of the novel antibiotic that will be required for future clinical trials. The subject invention also provides AST derivatives as a new class of antibiotics.
Synthesis of the organoarsenical antibiotic arsinothricin and derivatives thereof
The subject invention provides methods and procedures for synthesis and/or semi-synthesis of the novel antibiotic arsinothricin (AST) and derivatives. Arsinothricin (AST), a new broad-spectrum organoarsenical antibiotic, is a non-proteinogenic analog of glutamate that effectively inhibits glutamine synthetase. The subject invention provides chemical synthesis of an intermediate in the pathway of AST synthesis, hydroxyarsinothricin (AST-OH), which can be converted to AST by enzymatic methylation catalyzed by the ArsM As(III) S-adenosylmethionine methyltransferase. The methods provide a source of the novel antibiotic that will be required for future clinical trials. The subject invention also provides AST derivatives as a new class of antibiotics.