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PHOSPHONIUM COMPOUND AND PRODUCTION METHOD THEREFOR

外国特許コード F160008915
整理番号 S2016-0741-N0
掲載日 2016年12月22日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2015JP059857
国際公開番号 WO 2016072104
国際出願日 平成27年3月30日(2015.3.30)
国際公開日 平成28年5月12日(2016.5.12)
優先権データ
  • 特願2014-224986 (2014.11.5) JP
発明の名称 (英語) PHOSPHONIUM COMPOUND AND PRODUCTION METHOD THEREFOR
発明の概要(英語) The present invention provides a phosphonium compound indicated by formula (II). Also provided is a production method for a quaternary phosphonium compound labelled with positron emitting radionuclides, that includes a step in which: an electrophile indicated by formula (I) X1-CH2-A1 is reacted with a triphenylphosphine having at least one substituent labelled with positron emitting radionuclides on a benzene ring; and a quaternary phosphonium salt is obtained.
特許請求の範囲(英語) [claim1]
1. Formula (ii):
[In formula, Ar (1), Ar (2), and Ar (3) is the aryl which is possible to be substituted by the respective independence, B by the substituent of 1 or more where from (2) it is selected, here Ar (1), Ar (2), and Ar C [1-6] alkyl where (3) one the sign is done at least with radionuclide, with radionuclide the sign C [2-6] alkoxy which is done, with radionuclide the sign C [2-6] alkoxy C [1-6] alkyl which is done, with radionuclide the sign C [2-6] alkoxy C [2-6] alkoxy which is done, with radionuclide the sign C [2-6] alkoxy C which is done[2-6] With alkoxy C [1-6] alkyl, and radionuclide we are substituted with the substituent of 1 or more where it is selected from C [2-6] alkoxy C [2-6] alkoxy C [2-6] alkoxy which the sign is done;
A (1) is the aryl which is possible to be substituted C [2-10] [arukeniru], or B which is possible to be substituted C [1-10] alkyl which is possible to be substituted the hydrogen atom, by the substituent of 1 or more where it is selected from B (1), by the substituent of 1 or more where it is selected from B (1) by the substituent of 1 or more where it is selected from (2);
B (1), in the respective independence, the halogen atom, C [1-6] alkoxy, phenyl, and naphthyl to be, as for the said phenyl, and naphthyl, by the substituent of 1 or more where it is selected from C [1-6] alkyl, C [1-6] alkoxy, and the halogen atom may be substituted, here;
B (2), in the respective independence, the halogen atom, C [1-6] alkyl and C [1-6] alkoxy, C [1-6] alkyl thio and cyano, amino and C [1-6] alkyl amino, [ji] (C [1-6] alkyl) amino, nitro and hydroxy, or (C [1-3] alkoxy) carbonyl to be, as for the said alkyl, the alkoxy, and alkyl thio by the substituent of 1 or more where it is selected from the halogen atom may be substituted, here;
Ar (1), Ar (2), Ar (3) and A (1), and as for the substituent which is included in those, to be possible acid attaching salting to form;
X (-), entire electric charge - is the anion of 1]
So it is displayed, phosphonium chemical compound.
[claim2]
2. Radionuclide is positron discharge nuclide, in claim 1 the phosphonium chemical compound of statement.
[claim3]
3. Positron discharge nuclide (18) is F, in claim 2 the phosphonium chemical compound of statement.
[claim4]
4. A (1), is C [1-6] alkyl, phenyl or the phenyl C [1-4] alkyl which are possible to be substituted with the hydrogen atom and the halogen atom of 1 or more, here, as for the phenyl part of phenyl or phenyl C [1-4] alkyl, the halogen atom of 1 or more, C [1-6] alkyl and C [1-6] alkoxy, C [1-6] alkyl thio and cyano, amino and C [1-6] alkyl amino, [ji] (C [1-6] alkyl) amino, nitro and hydroxy, and (C [1-3] alkoxy) depending on the substituent of 1 or more where it is selected from carbonylIt is possible to be substituted, either of the claim 1-3 in 1 sections the phosphonium chemical compound of statement.
[claim5]
5. Benzyl - [4- (2- [(18) F] fluoro ethoxy) phenyl] - diphenyl phosphonium;
Benzyl - (4- [2- {2- (2- [(18) F] fluoro ethoxy) ethoxy} ethoxy] phenyl) - diphenyl phosphonium;
[4- (2- [(18) F] fluoro ethoxy) phenyl] - (4 - methoxycarbonyl phenyl) methyl - diphenyl phosphonium;
[4- (2- [(18) F] fluoro ethoxy) phenyl] - (4 - fluoro phenyl) methyl - diphenyl phosphonium;
[4- (2- [(18) F] fluoro ethoxy) phenyl] - (3,4,5 - [torihuruorohueniru]) methyl - diphenyl phosphonium;
(4 - [kurorohueniru]) methyl - [4- (2- [(18) F] fluoro ethoxy) phenyl] - diphenyl phosphonium;
[4- (2- [(18) F] fluoro ethoxy) phenyl] - (4 - methoxy phenyl) methyl - diphenyl phosphonium;
[4- (2- [(18) F] fluoro ethoxy) phenyl] - ([n]-penchiru) - diphenyl phosphonium;
[4- (2- [(18) F] fluoro ethoxy) phenyl] - (3 - phenyl propyl) - diphenyl phosphonium;
(*** -n-buchiru phenyl) methyl - [4- (2- [(18) F] fluoro ethoxy) phenyl] - diphenyl phosphonium;
(3 - Fluoro phenyl) methyl - [4- (2- [(18) F] fluoro ethoxy) phenyl] - diphenyl phosphonium;
[4- (2- [(18) F] fluoro ethoxy) phenyl] - [4- (trifluoromethyl thio) phenyl] methyl - diphenyl phosphonium;
[4- (2- [(18) F] fluoro ethoxy) phenyl] - (2 - methylphenyl) methyl - diphenyl phosphonium;
(3 - Cyano phenyl) methyl - [4- (2- [(18) F] fluoro ethoxy) phenyl] - diphenyl phosphonium;
[4- (2- [(18) F] fluoro ethoxy) phenyl] - methyl - diphenyl phosphonium;
Allyl - [4- (2- [(18) F] fluoro ethoxy) phenyl] - diphenyl phosphonium;
Benzyl - [3- (2- [(18) F] fluoro ethoxy) phenyl] - diphenyl phosphonium;
[3- (2- [(18) F] fluoro ethoxy) phenyl] - (4 - methoxy phenyl) methyl - diphenyl phosphonium;
[3- (2- [(18) F] fluoro ethoxy) phenyl] - (4 - methoxycarbonyl phenyl) methyl - diphenyl phosphonium;
[3- (2- [(18) F] fluoro ethoxy) phenyl] - (4 - fluoro phenyl) methyl - diphenyl phosphonium;
[3- (2- [(18) F] fluoro ethoxy) phenyl] - (3 - phenyl propyl) - diphenyl phosphonium;
(4 - [kurorohueniru]) methyl - [3- (2- [(18) F] fluoro ethoxy) phenyl] - diphenyl phosphonium;
[3- (2- [(18) F] fluoro ethoxy) phenyl] - (3,4,5 - [torihuruorohueniru]) methyl - diphenyl phosphonium;
Benzyl - [3- (3- [(18) F] [huruoropuropokishi]) phenyl] - diphenyl phosphonium;
Benzyl - [3- (4- [(18) F] [huruorobutokishi]) phenyl] - diphenyl phosphonium;
[3- (2- [(18) F] fluoro ethoxy) phenyl] - methyl - diphenyl phosphonium;
And
Benzyl - [2- (2- [(18) F] fluoro ethoxy) phenyl] - diphenyl phosphonium;
The empty the phosphonium which is selected is included, in claim 1 the phosphonium chemical compound of statement.
[claim6]
6. Benzyl - [4- (2- [(18) F] fluoro ethoxy) phenyl] - [jihueniruhosuhoniumuburomido];
Benzyl - [3- (2- [(18) F] fluoro ethoxy) phenyl] - [jihueniruhosuhoniumuburomido];
[3- (2- [(18) F] fluoro ethoxy) phenyl] - (4 - methoxy phenyl) methyl - [jihueniruhosuhoniumuburomido];
And
[3- (2- [(18) F] fluoro ethoxy) phenyl] - (3 - phenyl propyl) - [jihueniruhosuhoniumuburomido];
The empty it is selected, in claim 1 the phosphonium chemical compound of statement.
[claim7]
7. The radiopharmaceuticals which either of the claim 1-6 contain the phosphonium chemical compound of statement in 1 sections, use for imaging.
[claim8]
8. The radiopharmaceuticals which either of the claim 2-6 contain the phosphonium chemical compound of statement in 1 sections, use for PET imaging.
[claim9]
9. It is used for the imaging of the mitochondria, in claim 8 the radiopharmaceuticals for PET of statement.
[claim10]
10. The myocardium, it is used for the imaging of the tumor or brown adipose tissue, in claim 8 or 9 the radiopharmaceuticals for PET of statement.
[claim11]
11. Either of the claim 7-10 the morphism characteristic medical supply of statement is included in 1 sections, the disposable product.
[claim12]
12. Being production method of 4 class phosphonium chemical compounds which the sign are done with radionuclide,
Formula (i): X (1)-CH [2] - A (1)
[In formula, X (1) is the disconnection basis;
A (1) is the aryl which is possible to be substituted C [1-10] [arukeniru], or B which is possible to be substituted C [1-10] alkyl which is possible to be substituted the hydrogen atom, by the substituent of 1 or more where it is selected from B (1), by the substituent of 1 or more where it is selected from B (1) by the substituent of 1 or more where it is selected from (2);
B (1), in the respective independence, the halogen atom, C [1-6] alkoxy, phenyl, and naphthyl to be, as for the said phenyl, and naphthyl, by the substituent of 1 or more where it is selected from C [1-6] alkyl, C [1-6] alkoxy, and the halogen atom may be substituted, here;
B (2), in the respective independence, the halogen atom, C [1-6] alkyl and C [1-6] alkoxy, C [1-6] alkyl thio and cyano, amino and C [1-6] alkyl amino, [ji] (C [1-6] alkyl) amino, nitro and hydroxy, or (C [1-3] alkoxy) is carbonyl, the said alkyl, the alkoxy, and alkyl thio may be substituted here by the substituent of 1 or more where it is selected from the halogen atom]
So on benzene ring reacting the electrophilic medicine which is displayed, with the triphenylphosphine which possesses the substituent of 1 or more where the sign it is done with radionuclide, implication the process which obtains 4 class phosphonium salts;
Here with radionuclide the substituent of 1 or more where the sign it is done, with radionuclide C [1-6] alkyl which the sign is done, with radionuclide C [2-6] alkoxy which the sign is done, with radionuclide C [2-6] alkoxy C [1-6] alkyl which the sign is done, with radionuclide C [2-6] alkoxy C [2-6] alkoxy which the sign is done, with radionuclide with C [2-6] alkoxy C [2-6] alkoxy C [1-6] alkyl, and the radionuclide which the sign are done is selected from C [2-6] alkoxy C [2-6] alkoxy C [2-6] alkoxy which the sign is done;
Here the substituent of 1 or more where it is selected from B (2) furthermore it is possible to have possessed the said triphenylphosphine on benzene ring, aforementioned production method.
[claim13]
13. Radionuclide is positron discharge nuclide, in claim 12 production method of statement.
[claim14]
14. Positron discharge nuclide (18) is F, in claim 13 production method of statement.
[claim15]
15. X (1), the halogen atom, C [1-6] alkyl sulfonyl oxy which is possible to be substituted, or is the phenyl sulfonyl oxy which is possible to be substituted, either of the claim 12-14 in 1 sections production method of statement.
[claim16]
16. It does with the automatic synthetic device, either of the claim 12-15 in 1 sections production method of statement.
[claim17]
17. Formula (iii):
[In formula, Ar (1), Ar (2), and Ar (3) is, as defined in claim 1,]
So it is displayed, the phosphine compound.
[claim18]
18. Radionuclide (18) is F, in claim 17 the phosphine compound of statement.
[claim19]
19. Radionuclide was replaced to the non radioactive identical element, either of the claim 1-6 in 1 sections the phosphonium chemical compound of statement.
[claim20]
20. Either of the claim 3-6 the phosphonium chemical compound which (19) replaces (18) (18) F of the F sign phosphonium chemical compound of statement to F in 1 sections.
[claim21]
21. Formula (iii):
[In formula, Ar (1), Ar (2), and Ar (3) is the aryl which is possible to be substituted by the respective independence, B by the substituent of 1 or more where from (2) it is selected;
Here Ar (1), Ar (2), and Ar C [2-6] alkoxy C [2-6] alkoxy (3) at least one may be substituted C [2-6] alkoxy C [1-6] alkyl which is possible to be substituted C [2-6] alkoxy which is possible to be substituted C [1-6] alkyl which is possible to be substituted by the substituent of 1 or more where it is selected from L, by the substituent of 1 or more where it is selected from L, by the substituent of 1 or more where it is selected from L, by the substituent of 1 or more where it is selected from L, depending on the substituent of 1 or more where it is selected from LWe are substituted with the substituent of 1 or more where it is selected from C [2-6] alkoxy C [2-6] alkoxy C [2-6] alkoxy which is possible to be substituted by the substituent of 1 or more where it is selected from C [2-6] alkoxy C [2-6] alkoxy C [1-6] alkyl, and L which are possible to be substituted;
B (2), the halogen atom, C [1-6] alkyl and C [1-6] alkoxy, C [1-6] alkyl thio and cyano, amino and C [1-6] alkyl amino, [ji] (C [1-6] alkyl) amino, nitro and hydroxy, or (C [1-3] alkoxy) carbonyl to be, as for the said alkyl, the alkoxy, and alkyl thio by the substituent of 1 or more where it is selected from the halogen atom may be substituted, here;
L, bromine and iodine, the [p]-toruen sulfonyl oxy and the methane sulfonyl oxy, is [kurorometansuruhoniruokishi] or [torihuruorometansuruhoniruokishi]]
So it is displayed, the phosphine compound.
[claim22]
22. In claim 21 the chemical compound and radionuclide of statement, from claim 17 or the method of producing the phosphine compound of statement in 18.
[claim23]
23. Either of the claim 1-6 being the kit in order to produce the phosphonium chemical compound of statement in 1 sections, the aforementioned kit which includes the chemical compound of statement in claim 21 as the reagent.
[claim24]
24. Claim being the kit in order to produce 17 or the phosphine compound of statement in 18, the aforementioned kit which includes the chemical compound of statement in claim 21 as the reagent.
  • 出願人(英語)
  • ※2012年7月以前掲載分については米国以外のすべての指定国
  • TOHOKU UNIVERSITY
  • 発明者(英語)
  • FURUMOTO SHOZO
国際特許分類(IPC)
指定国 (WO201672104)
National States: AE AG AL AM AO AT AU AZ BA BB BG BH BN BR BW BY BZ CA CH CL CN CO CR CU CZ DE DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JP KE KG KN KP KR KZ LA LC LK LR LS LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PA PE PG PH PL PT QA RO RS RU RW SA SC SD SE SG SK SL SM ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW KM ML MR NE SN ST TD TG
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