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METHOD FOR PRODUCING EUSHEARILIDES

Foreign code F160008825
File No. (S2015-0093-N0)
Posted date Aug 10, 2016
Country WIPO
International application number 2015JP080469
International publication number WO 2016068220
Date of international filing Oct 28, 2015
Date of international publication May 6, 2016
Priority data
  • P2014-220491 (Oct 29, 2014) JP
Title METHOD FOR PRODUCING EUSHEARILIDES
Abstract Provided are: eushearilides; a method for producing eushearilides; a production intermediate; and a pharmaceutical composition containing eushearilides. By having the Wittig reaction process, Mukaiyama Aldol reaction process and Macrolactonizaion process serve as key processes, eushearilides represented by formula (I) are efficiently produced.
Scope of claims [claim1]
1. Production method of [yushieariraido] which include the process which is shown with the below-mentioned 1-10, are displayed with formula (i).
Process 1: Formula (I-1)
(In formula, P (1) displays the protective group.)
So the chemical compound which is displayed and,
Formula (I-2)
(In formula, R (1) the hydrogen atom or displays the hydrocarbon radical which is possible to be substituted, P (2) displays the protective group, X displays the halogen atom.)
So the chemical compound which is displayed the coupling doing under existing of the base, formula (I-3)
(In formula, R (1), P (1) and P (2) is the aforementioned sort.)
So the process which obtains the chemical compound which is displayed,
Process 2: Formula (I-3) with deviation from protecting the chemical compound which is displayed, formula (I-4)
(In formula, R (1) and P (2) is the aforementioned sort.)
So the process which obtains the chemical compound which is displayed,
Process 3: Formula (I-4) with oxidizing the chemical compound which is displayed, formula (I-5)
(In formula, R (1) and P (2) is the aforementioned sort.)
So the process which obtains the chemical compound which is displayed,
Process 4: Formula (I-5) with attaching the chemical compound which is displayed on the aldol reaction, formula (I-6)
(In formula, R (5) displays the hydrocarbon radical, R (1) and P (2) is the aforementioned sort.)
So the process which obtains the chemical compound which is displayed,
Process 5: Formula (I-6) with ester exchanging the chemical compound which is displayed, formula (I-7)
(In formula, R (1), R (5) and P (2) is the aforementioned sort.)
So the process which obtains the chemical compound which is displayed,
Process 6: Formula (I-7) with to protect the chemical compound which is displayed, deviation from protecting, formula (I-8)
(In formula, P (3) displays the protective group, R (1) and R (5) is the aforementioned sort.)
So the process which obtains the chemical compound which is displayed,
Process 7: Formula (I-8) with adding water disassembling the chemical compound which is displayed, formula (I-9)
(In formula, R (1) and P (3) is the aforementioned sort.)
So the process which obtains the chemical compound which is displayed,
Process 8: Formula (I-9) with the cyclization doing the chemical compound which is displayed, formula (I-10)
(In formula, R (1) and P (3) is the aforementioned sort.)
So the process which obtains the chemical compound which is displayed,
Process 9: Formula (I-10) with deviation from protecting the chemical compound which is displayed, formula (I-11)
(In formula, R (1) is the aforementioned sort.)
So the process which obtains the chemical compound which is displayed,
Process 10: Formula (I-11) with the phosphorus compound, continuously amine R (2) R (3) R (4) reacting the chemical compound which is displayed with N, formula (i)
(In formula, R (1) is the aforementioned sort, R (2), R (3) and R (4) the hydrogen atom or displays the hydrocarbon radical which is possible to be substituted in independence.)
So the process which obtains the chemical compound which is displayed.
[claim2]
2. Formula (Ia-11)
(In formula, R (1) the hydrogen atom or displays the hydrocarbon radical which is possible to be substituted.)
So the chemical compound which is displayed the phosphorus compound, continuously amine R (2) R (3) R (4) it depends on reacting with N, formula (Ia)
(In formula, R (1), R (2), R (3) and R (4) the hydrogen atom or displays the hydrocarbon radical which is possible to be substituted in independence.)
So production method of [yushieariraido] which are displayed.
[claim3]
3. Formula (Ia-11) with is displayed the chemical compound which, formula (Ia-9)
(In formula, R (1) is the aforementioned sort, P (3) displays the protective group.)
So 2 - methyl - 6 - reacting the chemical compound which is displayed with the nitro benzoic acid anhydride, formula (Ia-10)
(In formula, R (1) and P (3) is the aforementioned sort.)
So the process which obtains the chemical compound which is displayed,
It is obtained formula (Ia-10) with by the process which deviation from protects the chemical compound which is displayed, in claim 2 production method of statement.
[claim4]
4. Formula (Ia-9) with is displayed the chemical compound which, formula (I-1)
(In formula, P (1) displays the protective group.)
So the chemical compound which is displayed and,
Formula (Ia-2)
(In formula, R (1) the hydrogen atom or displays the hydrocarbon radical which is possible to be substituted, P (2) displays the protective group, X displays the halogen atom.)
So the chemical compound which is displayed the coupling doing under existing of the base, formula (Ia-3)
(In formula, R (1), P (1) and P (2) is the aforementioned sort.)
So the process which obtains the chemical compound which is displayed,
Formula (Ia-3) with deviation from protecting the chemical compound which is displayed, formula (Ia-4)
(In formula, R (1) and P (2) is the aforementioned sort.)
So the process which obtains the chemical compound which is displayed,
Formula (Ia-4) with oxidizing the chemical compound which is displayed, formula (Ia-5)
(In formula, R (1) and P (2) is the aforementioned sort.)
So the process which obtains the chemical compound which is displayed,
Formula (Ia-5) with attaching the chemical compound which is displayed on the aldol reaction, formula (Ia-6)
(In formula, R (5) displays the hydrocarbon radical, R (1) and P (2) is the aforementioned sort.)
So the process which obtains the chemical compound which is displayed,
Formula (Ia-6) with ester exchanging the chemical compound which is displayed, formula (Ia-7)
(In formula, R (1), R (5) and P (2) is the aforementioned sort.)
So the process which obtains the chemical compound which is displayed,
Formula (Ia-7) with to protect the chemical compound which is displayed, deviation from protecting, formula (Ia-8)
(In formula, P (3) displays the protective group, R (1) and R (5) is the aforementioned sort.)
So the process which obtains the chemical compound which is displayed,
It is obtained formula (Ia-8) with by the process which the chemical compound which is displayed adding water is disassembled, in claim 3 production method of statement.
[claim5]
5. Formula (Ia) with is displayed the [yushieariraido] chemical compound which, formula (A)
So claim 2-4 in each case is the chemical compound which is displayed in 1 sections production method of statement.
[claim6]
6. The chemical compound which is displayed with formula (ii).
(In formula, R (1) the hydrogen atom or displays the hydrocarbon radical which is possible to be substituted, P (3) displays the hydrogen atom or the protective group.)
However, in aforementioned formula (ii), R (1) is the methyl group, at the same time, the chemical compound where P (3) is the hydrogen atom or the benzyl basis is excluded.
[claim7]
7. Formula (A), (E) and (F) or (G) with the chemical compound which is displayed.
[claim8]
8. Formula (i)
(In formula, R (1), R (2), R (3) and R (4) the hydrogen atom or displays the hydrocarbon radical which is possible to be substituted in independence.)
So the chemical compound which is displayed (however, the below-mentioned chemical compound (D) is excluded.)The medicine composition which is contained.
[claim9]
9. In the claim 8 which is the anti-bacterial medicine the medicine composition of statement.
[claim10]
10. Is displayed with formula (i) the chemical compound which, the below-mentioned formula (A), (B), (C), (E) and (F), (G) or (H)
So in the claim 9 which is the chemical compound which is displayed or 10 the medicine composition of statement.
[claim11]
11. Formula (i)
(In formula, R (1), R (2), R (3) and R (4) the hydrogen atom or displays the hydrocarbon radical which is possible to be substituted in independence.)
So the anti-bacterial medicine for the tolerance germ which contains the chemical compound which is displayed.
[claim12]
12. Is displayed with formula (i) the chemical compound which, the below-mentioned formula (A), (B), (C), (D), (E) and (F), (G) or (H)
So in the claim 11 which is the chemical compound which is displayed the anti-bacterial medicine for the tolerance germ of statement.
[claim13]
13. The tolerance germ the [mechishirin] tolerance yellow staphylococcus (MRSA), the [bankomaishin] tolerance intestinal micrococcus (VRE) or the [bankomaishin] tolerance yellow staphylococcus (VRSA) in the claim 11 which is or 12 the anti-bacterial medicine for the tolerance germ of statement.
[claim14]
14. Formula (i)
(In formula, R (1), R (2), R (3) and R (4) the hydrogen atom or displays the hydrocarbon radical which is possible to be substituted in independence.)
So the remedy effective quantity of the medicine composition which contains the chemical compound which is displayed, the fact that it prescribes to the object which needs that is included, method of remedying or prevention the tolerance germ infection symptom.
[claim15]
15. Formula (i) in order to produce the anti-bacterial medicine for the tolerance germ
(In formula, R (1), R (2), R (3) and R (4) the hydrogen atom or displays the hydrocarbon radical which is possible to be substituted in independence.)
So use of the chemical compound which is displayed.
[claim16]
16. Formula (I-7)
(In formula, R (1) the hydrogen atom or displays the hydrocarbon radical which is possible to be substituted, P (2) displays the protective group, R (5) displays the hydrocarbon radical.)
So the chemical compound which is displayed is protected deviation from, the process which the cyclization is done next is included, formula (i)
(In formula, R (1) the hydrogen atom or displays the hydrocarbon radical which is possible to be substituted, R (2), R (3) and R (4) the hydrogen atom or displays the hydrocarbon radical which is possible to be substituted in independence.)
So production method of [yushieariraido] which are displayed.
[claim17]
17. Formula (I-7)
(In formula, R (1) the hydrogen atom or displays the hydrocarbon radical which is possible to be substituted, P (2) displays the protective group, R (5) displays the hydrocarbon radical.)
So deviation from protecting the chemical compound which is displayed, formula (I-12)
(In formula, R (1) is the aforementioned sort.)
So the process which obtains the chemical compound which is displayed,
The aforementioned system (I-12) with the cyclization doing the chemical compound which is displayed, formula (I-11)
(In formula, R (1) is the aforementioned sort.)
So the process which obtains the chemical compound which is displayed
In the claim 16 which is included production method of statement.
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • TOKYO UNIVERSITY OF SCIENCE EDUCATIONAL FOUNDATION
  • Inventor
  • SHIINA ISAMU
  • TONOI TAKAYUKI
IPC(International Patent Classification)
Specified countries 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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