Abstract: To provide a novel boron-containing compound. A compound represented by the following formula: wherein black circle represents B, white circles represent B—H; —R1 represents —(CH2)n-X1—R3 (n represents an integer of 0 to 6; X1 represents O, S, NH, S—S, O—CO, NHCO or SCO, or does not exist; R3 represents C6-C20 alkyl, hydroxy C6-C20 alkyl, amino C6-C20 alkyl, azido C6-C20 alkyl, hydroxycarbonyl C6-C20 alkyl, or the like), or a group having a repeating sequence of —(CH2)2—O— 3 times or more and 10 times or less and having a methyl group or an ethyl group at the end on the oxygen atom side; and —R2 is —(CH2)m-X2—R4 (m represents an integer from 0 to 8; X2 represents O, S, NH, S—S, O—CO, NHCO or SCO, or does not exist; and R4 represents a tumor recognition moiety), or does not exist are prepared and used.

Abstract: The present invention involves preparing compounds represented by the following formula: from a compound of the following formula: In these formulae: R1 represents a Br group, an iodine group, a Cl group, an NO2 group, or an NH2 group; R2 represents a halogen group, an NO2 group, an NH2 group, Sn(R6)3, N?N—NR7R8, OSO2R9, N R10R11, phenyliodonium, a heterocyclic group iodine, boric acid, or a borate ester; R30 represents a protective group PG1; R40 or R50 represent hydrogen, a protective group PG2, or C6H5(C6H5)C?N, in which NR40R50 are together.

Abstract: To provide a novel boron-containing compound. A compound represented by the following formula: wherein black circle represents B, white circles represent B—H; —R1 represents —(CH2)n-X1—R3 (n represents an integer of 0 to 6; X1 represents O, S, NH, S—S, O—CO, NHCO or SCO, or does not exist; R3 represents C6-C20 alkyl, hydroxy C6-C20 alkyl, amino C6-C20 alkyl, azido C6-C20 alkyl, hydroxycarbonyl C6-C20 alkyl, or the like), or a group having a repeating sequence of —(CH2)2—O— 3 times or more and 10 times or less and having a methyl group or an ethyl group at the end on the oxygen atom side; and —R2 is —(CH2)m-X2—R4 (m represents an integer from 0 to 8; X2 represents O, S, NH, S—S, O—CO, NHCO or SCO, or does not exist; and R4 represents a tumor recognition moiety), or does not exist are prepared and used.

Abstract: The present invention involves preparing compounds represented by the formula. (In the formula: R1 represents a Br group, an iodine group, a Cl group, an NO2 group, or an NH2 group; R2 represents a halogen group, an NO2 group, an NH2 group, Sn(R6)3, N?N—NR7R8, OSO2R9, NR10R11, phenyliodonium, a heterocyclic group iodine, boric acid, or a borate ester; R30 represents a protective group PG1; R40 or R50 represent hydrogen, a protective group PG2, or C6H5(C6H5)C?N, wherein NR40R50 are together.

Abstract: 18F-labeled 4-boronophenylalanine (BPA) can be produced by preparing and further processing a precursor of 18F-labeled BPA represented by the following formula: in which R1 represents a bromo group, an iodo group, a fluoro group, a diazaborinane derivative, BX3? or BX3?M+ (wherein X represents a halogen atom; and M+ represents a monovalent monoatomic cation, a polyatomic cation or a complex cation).

Abstract: The present invention involves preparing compounds represented by the following formula: from a compound of the following formula: In these formulae: R1 represents a Br group, an iodine group, a Cl group, an NO2 group, or an NH2 group; R2 represents a halogen group, an NO2 group, an NH2 group, Sn(R6)3, N?N—NR7R8, OSO2R9, N R10R11, phenyliodonium, a heterocyclic group iodine, boric acid, or a borate ester; R30 represents a protective group PG1; R40 or R50 represent hydrogen, a protective group PG2, or C6H5(C6H5)C?N, in which NR40R50 are together.

Abstract: 18F-labeled 4-boronophenylalanine (BPA) can be produced by preparing and further processing a precursor of 18F-labeled BPA represented by the following formula: in which R1 represents a bromo group, an iodo group, a fluoro group, a diazaborinane derivative, BX3? or BX3?M+ (wherein X represents a halogen atom; and M+ represents a monovalent monoatomic cation, a polyatomic cation or a complex cation).

Abstract: The present invention involves preparing compounds represented by the formula. (In the formula: R1 represents a Br group, an iodine group, a Cl group, an NO2 group, or an NH2 group; R2 represents a halogen group, an NO2 group, an NH2 group, Sn(R6)3, N?N—NR7R8, OSO2R9, NR10R11, phenyliodonium, a heterocyclic group iodine, boric acid, or a borate ester; R30 represents a protective group PG1; R40 or R50 represent hydrogen, a protective group PG2, or C6H5(C6H5)C?N, wherein NR40R50 are together.

Abstract: The purpose of the present invention is to provide a novel method for producing cereulide and a derivative thereof; an intermediate for cereulide; and a novel cereulide derivative. A novel didepsipeptide, a novel tetradepsipeptide, a novel octadepsipeptide and a novel dodecadepsipeptide are prepared. A linear precursor of cereulide or a derivative thereof, which is composed of any one of the novel depsipeptides, is cyclized by forming an intramolecular amide bond.

Abstract: Provided are: a novel chiral 4-boronophenylalanine (BPA) derivative; a method for producing the derivative; and a method for producing 18F-2-fluoro-4-borono-L-phenylalanine (18F-labeled BPA; 18F-BPA) using the derivative. A compound represented by formula (1) is prepared. In the formula, R represents BR3R4, BX3? or BX3?M+ (wherein X represents a halogen atom, and M+ represents a monovalent monoatomic cation, a polyatomic cation or a complex cation); R1 represents a hydrogen atom or a protecting group PG1; R2 represents a hydrogen atom or a protecting group PG2; R3 and R4 independently represent OH, or R3, R4 and B together form a ring that serves as a protecting group; and Y represents a halogen atom, NO2, NH2, Sn(R6)3, N?N—NR7R8, OSO2R9, NR10R11, a substituted or unsubstituted phenyliodo group or a substituted or unsubstituted heterocyclic iodo group. The compound is reacted with a fluorination reagent to prepare 18F-labeled BPA.

Abstract: Provided are: a novel chiral 4-boronophenylalanine (BPA) derivative; a method for producing the derivative; and a method for producing 18F-2-fluoro-4-borono-L-phenylalanine (18F-labeled BPA; 18F-BPA) using the derivative. A compound represented by formula (1) is prepared. In the formula, R represents BR3R4, BX3? or BX3?M+ (wherein X represents a halogen atom, and M+ represents a monovalent monoatomic cation, a polyatomic cation or a complex cation); R1 represents a hydrogen atom or a protecting group PG1; R2 represents a hydrogen atom or a protecting group PG2; R3 and R4 independently represent OH, or R3, R4 and B together form a ring that serves as a protecting group; and Y represents a halogen atom, NO2, NH2, Sn(R6)3, N?N—NR7R8, OSO2R9, NR10R11, a substituted or unsubstituted phenyliodo group or a substituted or unsubstituted heterocyclic iodo group. The compound is reacted with a fluorination reagent to prepare 18F-labeled BPA.

Abstract: The purpose of the present invention is to provide a novel method for producing cereulide and a derivative thereof; an intermediate for cereulide; and a novel cereulide derivative. A novel didepsipeptide, a novel tetradepsipeptide, a novel octadepsipeptide and a novel dodecadepsipeptide are prepared. A linear precursor of cereulide or a derivative thereof, which is composed of any one of the novel depsipeptides, is cyclized by forming an intramolecular amide bond.

Abstract: The purpose of the present invention is to provide a novel boron-containing compound utilizable in BNCT and so on and a process for preparing same. According to the process, a boron compounds having an amino acid skeleton containing cyclo-type rings or a pharmaceutically acceptable salt thereof is prepared, said boron compound being represented by general formula (I) [wherein l is an integer of 1 to 6; m is 0, 1, or 2; and n is 0, 1 or 2].

Abstract: The present invention is a compound having a structure represented by the following formula (1): and an antibody to BSH obtained by using the compound as a hapten and using a complex of the hapten and a high-molecular compound as an antigen. By using the present invention, it becomes possible to provide a hapten compound for preparing an antibody recognizing BSH highly sensitively and highly selectively, an antibody to BSH, as well as a kit for measuring BSH and an immunological measuring method having high sensitivity and excellent in quantitative property using the antibody.

Abstract: The purpose of the present invention is to provide a novel boron-containing compound utilizable in BNCT and so on and a process for preparing same. According to the process, a boron compounds having an amino acid skeleton containing cyclo-type rings or a pharmaceutically acceptable salt thereof is prepared, said boron compound being represented by general formula (I) [wherein l is an integer of 1 to 6; m is 0, 1, or 2; and n is 0, 1 or 2].

Abstract: Disclosed is the method for producing an optically active BSH amino acid, which comprises a step of reacting an optically active a-amino acid derivative having a halogen in a side chain with a cyanoethyl BSH compound represented by formula (1). An optically active BSH amino acid obtained by the method is also disclosed.

Abstract: Disclosed is a method for producing a BSH derivative, which comprises a step of addition-reacting BSH with an ?,?-unsaturated nitrile compound in the presence of a base. Various BSH derivatives obtained by the method are also disclosed.

Abstract: Disclosed is the method for producing an optically active BSH amino acid, which comprises a step of reacting an optically active a-amino acid derivative having a halogen in a side chain with a cyanoethyl BSH compound represented by formula (1). An optically active BSH amino acid obtained by the method is also disclosed.

Abstract: The present invention is a compound having a structure represented by the following formula (1): and an antibody to BSH obtained by using the compound as a hapten and using a complex of the hapten and a high-molecular compound as an antigen. By using the present invention, it becomes possible to provide a hapten compound for preparing an antibody recognizing BSH highly sensitively and highly selectively, an antibody to BSH, as well as a kit for measuring BSH and an immunological measuring method having high sensitivity and excellent in quantitative property using the antibody.