JPS6360038B2 - - Google Patents
Info
- Publication number
- JPS6360038B2 JPS6360038B2 JP61016008A JP1600886A JPS6360038B2 JP S6360038 B2 JPS6360038 B2 JP S6360038B2 JP 61016008 A JP61016008 A JP 61016008A JP 1600886 A JP1600886 A JP 1600886A JP S6360038 B2 JPS6360038 B2 JP S6360038B2
- Authority
- JP
- Japan
- Prior art keywords
- dimethyl
- norpregna
- diene
- methoxy
- acid
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired
Links
- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 claims description 16
- 239000002253 acid Substances 0.000 claims description 13
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 9
- 229910021529 ammonia Inorganic materials 0.000 claims description 8
- WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical compound [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 claims description 6
- YZCKVEUIGOORGS-NJFSPNSNSA-N Tritium Chemical compound [3H] YZCKVEUIGOORGS-NJFSPNSNSA-N 0.000 claims description 6
- 229910052739 hydrogen Inorganic materials 0.000 claims description 6
- 239000001257 hydrogen Substances 0.000 claims description 6
- 229910052744 lithium Inorganic materials 0.000 claims description 6
- 229910052722 tritium Inorganic materials 0.000 claims description 6
- 125000000217 alkyl group Chemical group 0.000 claims description 5
- VAYGXNSJCAHWJZ-UHFFFAOYSA-N dimethyl sulfate Chemical compound COS(=O)(=O)OC VAYGXNSJCAHWJZ-UHFFFAOYSA-N 0.000 claims description 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 5
- 150000003431 steroids Chemical class 0.000 claims description 5
- 238000000034 method Methods 0.000 claims description 4
- 239000007864 aqueous solution Substances 0.000 claims description 3
- 125000004432 carbon atom Chemical group C* 0.000 claims description 3
- 239000003054 catalyst Substances 0.000 claims description 3
- GRWVQDDAKZFPFI-UHFFFAOYSA-H chromium(III) sulfate Chemical compound [Cr+3].[Cr+3].[O-]S([O-])(=O)=O.[O-]S([O-])(=O)=O.[O-]S([O-])(=O)=O GRWVQDDAKZFPFI-UHFFFAOYSA-H 0.000 claims description 3
- JUJWROOIHBZHMG-UHFFFAOYSA-O pyridinium Chemical compound C1=CC=[NH+]C=C1 JUJWROOIHBZHMG-UHFFFAOYSA-O 0.000 claims description 3
- 150000002431 hydrogen Chemical class 0.000 claims description 2
- 230000002194 synthesizing effect Effects 0.000 claims description 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 2
- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims description 2
- SQWBBFUHZKCYCT-YSTOQKLRSA-N (8s,13s,14s,17s)-17-acetyl-13-methyl-2,6,7,8,11,12,14,15,16,17-decahydro-1h-cyclopenta[a]phenanthren-3-one Chemical compound C1CC2=CC(=O)CCC2=C2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 SQWBBFUHZKCYCT-YSTOQKLRSA-N 0.000 claims 1
- 238000005533 tritiation Methods 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 description 38
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 27
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 27
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 21
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 20
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 19
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 18
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 14
- 239000000203 mixture Substances 0.000 description 13
- WFDIJRYMOXRFFG-UHFFFAOYSA-N Acetic anhydride Chemical compound CC(=O)OC(C)=O WFDIJRYMOXRFFG-UHFFFAOYSA-N 0.000 description 12
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 12
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 12
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 12
- 238000003756 stirring Methods 0.000 description 12
- 239000011541 reaction mixture Substances 0.000 description 11
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Natural products C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 description 7
- 239000000243 solution Substances 0.000 description 7
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 7
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 6
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 6
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 6
- 239000000377 silicon dioxide Substances 0.000 description 6
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 6
- 230000007935 neutral effect Effects 0.000 description 5
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 4
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 4
- 230000015572 biosynthetic process Effects 0.000 description 4
- 239000003795 chemical substances by application Substances 0.000 description 4
- INQOMBQAUSQDDS-UHFFFAOYSA-N iodomethane Chemical compound IC INQOMBQAUSQDDS-UHFFFAOYSA-N 0.000 description 4
- 229910052700 potassium Inorganic materials 0.000 description 4
- 239000011591 potassium Substances 0.000 description 4
- 229960003387 progesterone Drugs 0.000 description 4
- 239000000186 progesterone Substances 0.000 description 4
- 239000007858 starting material Substances 0.000 description 4
- 238000003786 synthesis reaction Methods 0.000 description 4
- BUDQDWGNQVEFAC-UHFFFAOYSA-N Dihydropyran Chemical compound C1COC=CC1 BUDQDWGNQVEFAC-UHFFFAOYSA-N 0.000 description 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 3
- 239000012141 concentrate Substances 0.000 description 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 3
- -1 methyl halide Chemical class 0.000 description 3
- 230000011987 methylation Effects 0.000 description 3
- 238000007069 methylation reaction Methods 0.000 description 3
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 3
- 239000011347 resin Substances 0.000 description 3
- 229920005989 resin Polymers 0.000 description 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- 238000006027 Birch reduction reaction Methods 0.000 description 2
- FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Chemical compound CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 2
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 2
- WGLPBDUCMAPZCE-UHFFFAOYSA-N Trioxochromium Chemical compound O=[Cr](=O)=O WGLPBDUCMAPZCE-UHFFFAOYSA-N 0.000 description 2
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 description 2
- 150000007513 acids Chemical class 0.000 description 2
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 description 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 description 2
- 238000010828 elution Methods 0.000 description 2
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 description 2
- 238000001914 filtration Methods 0.000 description 2
- 230000000887 hydrating effect Effects 0.000 description 2
- KQNPFQTWMSNSAP-UHFFFAOYSA-N isobutyric acid Chemical compound CC(C)C(O)=O KQNPFQTWMSNSAP-UHFFFAOYSA-N 0.000 description 2
- BRMYZIKAHFEUFJ-UHFFFAOYSA-L mercury diacetate Chemical compound CC(=O)O[Hg]OC(C)=O BRMYZIKAHFEUFJ-UHFFFAOYSA-L 0.000 description 2
- BDAGIHXWWSANSR-UHFFFAOYSA-N methanoic acid Natural products OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 description 2
- 239000003208 petroleum Substances 0.000 description 2
- 229920001467 poly(styrenesulfonates) Polymers 0.000 description 2
- 102000005962 receptors Human genes 0.000 description 2
- 108020003175 receptors Proteins 0.000 description 2
- 238000010992 reflux Methods 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 238000010189 synthetic method Methods 0.000 description 2
- ZDPHROOEEOARMN-UHFFFAOYSA-N undecanoic acid Chemical compound CCCCCCCCCCC(O)=O ZDPHROOEEOARMN-UHFFFAOYSA-N 0.000 description 2
- 238000005406 washing Methods 0.000 description 2
- DXBHBZVCASKNBY-UHFFFAOYSA-N 1,2-Benz(a)anthracene Chemical compound C1=CC=C2C3=CC4=CC=CC=C4C=C3C=CC2=C1 DXBHBZVCASKNBY-UHFFFAOYSA-N 0.000 description 1
- NWUYHJFMYQTDRP-UHFFFAOYSA-N 1,2-bis(ethenyl)benzene;1-ethenyl-2-ethylbenzene;styrene Chemical compound C=CC1=CC=CC=C1.CCC1=CC=CC=C1C=C.C=CC1=CC=CC=C1C=C NWUYHJFMYQTDRP-UHFFFAOYSA-N 0.000 description 1
- JKTCBAGSMQIFNL-UHFFFAOYSA-N 2,3-dihydrofuran Chemical compound C1CC=CO1 JKTCBAGSMQIFNL-UHFFFAOYSA-N 0.000 description 1
- LBLYYCQCTBFVLH-UHFFFAOYSA-N 2-Methylbenzenesulfonic acid Chemical compound CC1=CC=CC=C1S(O)(=O)=O LBLYYCQCTBFVLH-UHFFFAOYSA-N 0.000 description 1
- WLJVXDMOQOGPHL-PPJXEINESA-N 2-phenylacetic acid Chemical compound O[14C](=O)CC1=CC=CC=C1 WLJVXDMOQOGPHL-PPJXEINESA-N 0.000 description 1
- WTRRIQCGCGCMQA-CBZIJGRNSA-N 3-Hydroxyestra-1,3,5(10),6-tetraen-17-one Chemical compound OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3C=CC2=C1 WTRRIQCGCGCMQA-CBZIJGRNSA-N 0.000 description 1
- XMIIGOLPHOKFCH-UHFFFAOYSA-N 3-phenylpropionic acid Chemical compound OC(=O)CCC1=CC=CC=C1 XMIIGOLPHOKFCH-UHFFFAOYSA-N 0.000 description 1
- OSWFIVFLDKOXQC-UHFFFAOYSA-N 4-(3-methoxyphenyl)aniline Chemical compound COC1=CC=CC(C=2C=CC(N)=CC=2)=C1 OSWFIVFLDKOXQC-UHFFFAOYSA-N 0.000 description 1
- OTLNPYWUJOZPPA-UHFFFAOYSA-N 4-nitrobenzoic acid Chemical compound OC(=O)C1=CC=C([N+]([O-])=O)C=C1 OTLNPYWUJOZPPA-UHFFFAOYSA-N 0.000 description 1
- ARSRBNBHOADGJU-UHFFFAOYSA-N 7,12-dimethyltetraphene Chemical compound C1=CC2=CC=CC=C2C2=C1C(C)=C(C=CC=C1)C1=C2C ARSRBNBHOADGJU-UHFFFAOYSA-N 0.000 description 1
- 102100032323 Corticosteroid-binding globulin Human genes 0.000 description 1
- YYLLIJHXUHJATK-UHFFFAOYSA-N Cyclohexyl acetate Chemical compound CC(=O)OC1CCCCC1 YYLLIJHXUHJATK-UHFFFAOYSA-N 0.000 description 1
- VFZRZRDOXPRTSC-UHFFFAOYSA-N DMBA Natural products COC1=CC(OC)=CC(C=O)=C1 VFZRZRDOXPRTSC-UHFFFAOYSA-N 0.000 description 1
- ZAFNJMIOTHYJRJ-UHFFFAOYSA-N Diisopropyl ether Chemical compound CC(C)OC(C)C ZAFNJMIOTHYJRJ-UHFFFAOYSA-N 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- KDLHZDBZIXYQEI-UHFFFAOYSA-N Palladium Chemical compound [Pd] KDLHZDBZIXYQEI-UHFFFAOYSA-N 0.000 description 1
- 241000220324 Pyrus Species 0.000 description 1
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 description 1
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical class [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 1
- 108010011095 Transcortin Proteins 0.000 description 1
- CIHXIRAAMAUYLZ-UHFFFAOYSA-N [K+].[K+].[C-]#[C-] Chemical group [K+].[K+].[C-]#[C-] CIHXIRAAMAUYLZ-UHFFFAOYSA-N 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 125000004423 acyloxy group Chemical group 0.000 description 1
- 229910052783 alkali metal Inorganic materials 0.000 description 1
- 150000001340 alkali metals Chemical class 0.000 description 1
- YNQLUTRBYVCPMQ-UHFFFAOYSA-N alpha-methyl toluene Natural products CCC1=CC=CC=C1 YNQLUTRBYVCPMQ-UHFFFAOYSA-N 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 239000002585 base Substances 0.000 description 1
- 230000005587 bubbling Effects 0.000 description 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- IJOOHPMOJXWVHK-UHFFFAOYSA-N chlorotrimethylsilane Chemical compound C[Si](C)(C)Cl IJOOHPMOJXWVHK-UHFFFAOYSA-N 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- HJZLEGIHUQOJBA-UHFFFAOYSA-N cyclohexane propionic acid Chemical compound OC(=O)CCC1CCCCC1 HJZLEGIHUQOJBA-UHFFFAOYSA-N 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 239000003480 eluent Substances 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 235000019253 formic acid Nutrition 0.000 description 1
- 229910052736 halogen Inorganic materials 0.000 description 1
- 150000002367 halogens Chemical class 0.000 description 1
- 239000005457 ice water Substances 0.000 description 1
- 239000000543 intermediate Substances 0.000 description 1
- 239000003456 ion exchange resin Substances 0.000 description 1
- 229920003303 ion-exchange polymer Polymers 0.000 description 1
- 238000006317 isomerization reaction Methods 0.000 description 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 238000002844 melting Methods 0.000 description 1
- 230000008018 melting Effects 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 239000012074 organic phase Substances 0.000 description 1
- 235000021017 pears Nutrition 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 102000003998 progesterone receptors Human genes 0.000 description 1
- 108090000468 progesterone receptors Proteins 0.000 description 1
- 235000019260 propionic acid Nutrition 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
- 238000001953 recrystallisation Methods 0.000 description 1
- 239000012260 resinous material Substances 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 229910052938 sodium sulfate Inorganic materials 0.000 description 1
- 235000011152 sodium sulphate Nutrition 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 238000004809 thin layer chromatography Methods 0.000 description 1
- JBWKIWSBJXDJDT-UHFFFAOYSA-N triphenylmethyl chloride Chemical compound C=1C=CC=CC=1C(C=1C=CC=CC=1)(Cl)C1=CC=CC=C1 JBWKIWSBJXDJDT-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0081—Substituted in position 17 alfa and 17 beta
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0081—Substituted in position 17 alfa and 17 beta
- C07J1/0088—Substituted in position 17 alfa and 17 beta the substituent in position 17 alfa being an unsaturated hydrocarbon group
- C07J1/0096—Alkynyl derivatives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
- C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
- C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
- C07J7/004—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa
- C07J7/0045—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa not substituted in position 16
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Steroid Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Description
ãçºæã®è©³çŽ°ãªèª¬æã
æ¬çºæã®äž»é¡ã¯ã次ã®äžè¬åŒ
ïŒããã§ïŒ²ã¯æ°ŽçŽ ååãïŒãïŒåã®ççŽ ååãå«
æããã¢ã«ãã«åºåã¯ããã©ããããã©ãã«ãã
ãªãã«è¥ããã¯ããªã¡ãã«ã·ãªã«åºãè¡šããïŒã®
ã¹ããã€ããããªããŠã æšèä»ãã®çœ®æã¹ããã€
ãèªå°äœãåæããæ¹æ³ã«ããã
æããã¢ã«ãã«åºåã¯ããã©ããããã©ãã«ãã
ãªãã«è¥ããã¯ããªã¡ãã«ã·ãªã«åºãè¡šããïŒã®
ã¹ããã€ããããªããŠã æšèä»ãã®çœ®æã¹ããã€
ãèªå°äœãåæããæ¹æ³ã«ããã
åŒã«ãããŠããã¢ã«ãã«åºãè¡šãããšã
ã¯ãããã¯ãäŸãã°ã¡ãã«ããšãã«ããããã«ã
ã€ãœãããã«ãããã«ãsecâããã«åã¯ïœâã
ãã«åºã§ããã
ã¯ãããã¯ãäŸãã°ã¡ãã«ããšãã«ããããã«ã
ã€ãœãããã«ãããã«ãsecâããã«åã¯ïœâã
ãã«åºã§ããã
åŒã®ååç©ã®äžã§ããç¹ã«äžèšã®ãã®ããã
ãããã
ãããã
17αïŒ21âãžã¡ãã«â19âãã«ãã¬ã°ãâïŒïŒ
ïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâãªãŒã«â20âãª
ã³ã 17αïŒ21âãžã¡ãã«â19âãã«ãã¬ã°ãâïŒïŒ
ïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâã¡ããã·â20â
ãªã³ãåã³ 17αïŒ21âãžã¡ãã«â19âãã«ãã¬ã°ãâïŒïŒ
ïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâïŒÎ±âããã©ã
ãããã©ãã«ãªãã·ïŒâ20âãªã³ã
ïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâãªãŒã«â20âãª
ã³ã 17αïŒ21âãžã¡ãã«â19âãã«ãã¬ã°ãâïŒïŒ
ïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâã¡ããã·â20â
ãªã³ãåã³ 17αïŒ21âãžã¡ãã«â19âãã«ãã¬ã°ãâïŒïŒ
ïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâïŒÎ±âããã©ã
ãããã©ãã«ãªãã·ïŒâ20âãªã³ã
äžè¬åŒã®ååç©ã¯ãããªããŠã æšèä»ãã®çœ®
æã¹ããã€ãèªå°äœã®åæçšåºçºç©è³ªãšããŠæçš
ã§ããã
æã¹ããã€ãèªå°äœã®åæçšåºçºç©è³ªãšããŠæçš
ã§ããã
åèšã®äžè¬åŒã«çžåœããååç©ã¯æ¬¡ã®ããã«
補é ãããã
補é ãããã
ãã®æ¹æ³ã¯ããšããã«åå€ããšã¹ãã©âïŒïŒ
ïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâãªãŒã«â17âãª
ã³ã«åå¿ãããŠ17αâãšããã«ãšã¹ãã©âïŒïŒ
ïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒïŒ17βâãžãªãŒã«
ã圢æãããããé žã«ããåã¯é žã®å®èœæ§èªå°äœ
ã«ãããšã¹ãã«åããŠ17αâãšããã«ãšã¹ãã©â
ïŒïŒïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒïŒ17βâãžã¢
ã·ã«ãªãã·ãåŸãããã«æ°Žåå€ãäœçšãããçã
ã17αâã¢ã»ãã«ãšã¹ãã©âïŒïŒïŒïŒïŒ(10)ïŒïŒâ
ããã©ãšã³âïŒïŒ17βâãžã¢ã·ã«ãªãã·ã«ã¢ã³ã¢
ãã¢äžã®ã¢ã«ã«ãªéå±åã³ããã²ã³åã¡ãã«ãå
å¿ãããŠ17äœçœ®ã®ã¡ãã«åãš17äœçœ®ã®ã¢ã»ãã«å®
èœåºã®ç°æ§åãåæã«è¡ãªãããåŸããã17αâ
ã¡ãã«â19âãã«ãã¬ã°ãâïŒïŒïŒïŒïŒ(10)ïŒïŒâ
ããã©ãšã³âïŒâã¢ã·ã«ãªãã·â20âãªã³ã匷塩
åºæ°Žæº¶æ¶²ã«ããããåãã17αâã¡ãã«â19âã
ã«ãã¬ã°ãâïŒïŒïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒ
âãªãŒã«â20âãªã³ã®ïŒäœçœ®ã®ããããã·ã«å®èœ
åºããžããããã©ã³ãå¡©åããªãã«è¥ããã¯å¡©å
ããªã¡ãã«ã·ãªã«åã¯ã¢ã«ãã«åºãçºçããç©è³ª
ãããªã矀ããéžã°ããèªå°äœã«ãã€ãŠãããã¯
ããŠ17αâã¡ãã«â19âãã«ãã¬ã°ãâïŒïŒïŒïŒ
ïŒ(10)ïŒïŒâããã©ãšã³âïŒâROâ20âãªã³ïŒïŒ²
ã¯äžã«èšèŒã®æå³ãæããããã ããæ°ŽçŽ ã¯é€
ãïŒãåŸããã®21äœçœ®ã®ã¡ãã«åã觊åªã®ååšäž
ã«ããã²ã³åã¡ãã«ã«ãã€ãŠè¡ãªã€ãŠ17αïŒ21â
ãžã¡ãã«â19âãã«ãã¬ã°ãâïŒïŒïŒïŒïŒ(10)ïŒïŒ
âããã©ãšã³âïŒâROâ20âãªã³ãå³ã¡ïŒ²ãæ°Ž
çŽ ã§ãªãäžè¬åŒã®ååç©ãåŸããã®ïŒäœçœ®ã®ã
ãããã·ã«å®èœåºãé žã®äœçšã«ããéé¢ãããŠïŒ²
ãæ°ŽçŽ ååãè¡šããäžè¬åŒã®ååç©ãåŸãå¿ èŠ
ãªãã°ïŒäœçœ®ã®ããããã·ã«å®èœåºããšãŒãã«å
ããŠïŒ²ãæ°ŽçŽ ã§ãªãäžè¬åŒã®ååç©ãåŸãããš
ãç¹åŸŽãšãããã®ã§ããã
ïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâãªãŒã«â17âãª
ã³ã«åå¿ãããŠ17αâãšããã«ãšã¹ãã©âïŒïŒ
ïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒïŒ17βâãžãªãŒã«
ã圢æãããããé žã«ããåã¯é žã®å®èœæ§èªå°äœ
ã«ãããšã¹ãã«åããŠ17αâãšããã«ãšã¹ãã©â
ïŒïŒïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒïŒ17βâãžã¢
ã·ã«ãªãã·ãåŸãããã«æ°Žåå€ãäœçšãããçã
ã17αâã¢ã»ãã«ãšã¹ãã©âïŒïŒïŒïŒïŒ(10)ïŒïŒâ
ããã©ãšã³âïŒïŒ17βâãžã¢ã·ã«ãªãã·ã«ã¢ã³ã¢
ãã¢äžã®ã¢ã«ã«ãªéå±åã³ããã²ã³åã¡ãã«ãå
å¿ãããŠ17äœçœ®ã®ã¡ãã«åãš17äœçœ®ã®ã¢ã»ãã«å®
èœåºã®ç°æ§åãåæã«è¡ãªãããåŸããã17αâ
ã¡ãã«â19âãã«ãã¬ã°ãâïŒïŒïŒïŒïŒ(10)ïŒïŒâ
ããã©ãšã³âïŒâã¢ã·ã«ãªãã·â20âãªã³ã匷塩
åºæ°Žæº¶æ¶²ã«ããããåãã17αâã¡ãã«â19âã
ã«ãã¬ã°ãâïŒïŒïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒ
âãªãŒã«â20âãªã³ã®ïŒäœçœ®ã®ããããã·ã«å®èœ
åºããžããããã©ã³ãå¡©åããªãã«è¥ããã¯å¡©å
ããªã¡ãã«ã·ãªã«åã¯ã¢ã«ãã«åºãçºçããç©è³ª
ãããªã矀ããéžã°ããèªå°äœã«ãã€ãŠãããã¯
ããŠ17αâã¡ãã«â19âãã«ãã¬ã°ãâïŒïŒïŒïŒ
ïŒ(10)ïŒïŒâããã©ãšã³âïŒâROâ20âãªã³ïŒïŒ²
ã¯äžã«èšèŒã®æå³ãæããããã ããæ°ŽçŽ ã¯é€
ãïŒãåŸããã®21äœçœ®ã®ã¡ãã«åã觊åªã®ååšäž
ã«ããã²ã³åã¡ãã«ã«ãã€ãŠè¡ãªã€ãŠ17αïŒ21â
ãžã¡ãã«â19âãã«ãã¬ã°ãâïŒïŒïŒïŒïŒ(10)ïŒïŒ
âããã©ãšã³âïŒâROâ20âãªã³ãå³ã¡ïŒ²ãæ°Ž
çŽ ã§ãªãäžè¬åŒã®ååç©ãåŸããã®ïŒäœçœ®ã®ã
ãããã·ã«å®èœåºãé žã®äœçšã«ããéé¢ãããŠïŒ²
ãæ°ŽçŽ ååãè¡šããäžè¬åŒã®ååç©ãåŸãå¿ èŠ
ãªãã°ïŒäœçœ®ã®ããããã·ã«å®èœåºããšãŒãã«å
ããŠïŒ²ãæ°ŽçŽ ã§ãªãäžè¬åŒã®ååç©ãåŸãããš
ãç¹åŸŽãšãããã®ã§ããã
奜ãŸããå®æœæ¡ä»¶äžã§ã¯ãäžèšã®æ¹æ³ã¯æ¬¡ã®ç¹
ã«ãã€ãŠç¹åŸŽã¥ããããã
ã«ãã€ãŠç¹åŸŽã¥ããããã
ãšããã«åå€ã¯ã«ãªãŠã ã¢ã»ããªãã§ãããã
ããŠãã®åŠçã¯ã«ãªãŠã ïœâããã©ãŒãã®ååšäž
ã«ããã©ããããã©ã³äžã§è¡ãªãããã
ããŠãã®åŠçã¯ã«ãªãŠã ïœâããã©ãŒãã®ååšäž
ã«ããã©ããããã©ã³äžã§è¡ãªãããã
ïŒåã³17äœçœ®ã®ããããã·ã«å®èœåºã¯ç¡æ°Žé
¢é
ž
ã«ãããšã¹ãã«åããããããŠãã®åŠçã¯ïœâã
ã«ãšã³ã¹ã«ãã³é žã®ååšäžã«è¡ãªããããïŒã18
åã®ççŽ ååãå«æããé žãäžã§ããé žãããã
ãªã³é žãé ªé žãã€ãœé ªé žããŠã³ãã·ã«é žãã·ã¯ã
ãã³ãã«è¥ããã¯ã·ã¯ãããã·ã«é ¢é žãã·ã¯ãã
ã³ãã«è¥ããã¯ã·ã¯ãããã·ã«ããããªã³é žãã
ãšãã«é ¢é žãããšãã«ããããªã³é žãïœâããã
å®æ¯éŠé žåã¯ããªãã«ãªã«é ¢é žã®ãããªãã®ä»ã®
é žåã¯ãã®å®èœæ§èªå°äœãçšããããšãã§ããã
ã«ãããšã¹ãã«åããããããŠãã®åŠçã¯ïœâã
ã«ãšã³ã¹ã«ãã³é žã®ååšäžã«è¡ãªããããïŒã18
åã®ççŽ ååãå«æããé žãäžã§ããé žãããã
ãªã³é žãé ªé žãã€ãœé ªé žããŠã³ãã·ã«é žãã·ã¯ã
ãã³ãã«è¥ããã¯ã·ã¯ãããã·ã«é ¢é žãã·ã¯ãã
ã³ãã«è¥ããã¯ã·ã¯ãããã·ã«ããããªã³é žãã
ãšãã«é ¢é žãããšãã«ããããªã³é žãïœâããã
å®æ¯éŠé žåã¯ããªãã«ãªã«é ¢é žã®ãããªãã®ä»ã®
é žåã¯ãã®å®èœæ§èªå°äœãçšããããšãã§ããã
17äœçœ®ã®ãšããã«å®èœåºã®æ°Žåå€ã¯é
¢é
žç¬¬äºæ°Ž
éã§æŽ»æ§åãããããŠãšãã¯ã¹50æš¹èã§ãããã
ããŠåŠçã¯ãšã¿ããŒã«äžã§è¡ãªãããã
éã§æŽ»æ§åãããããŠãšãã¯ã¹50æš¹èã§ãããã
ããŠåŠçã¯ãšã¿ããŒã«äžã§è¡ãªãããã
17äœçœ®ã®ã¡ãã«ååã³ã¢ã»ãã«å®èœåºã®ç°æ§å
ã¯ãã¢ã³ã¢ãã¢äžã®ãªããŠã åã³ããåã¡ãã«ã«
ãã€ãŠåæã«è¡ãªããããããŠåŠçã¯å·åŽäžã«ã
ãã©ããããã©ã³äžã§è¡ãªãããã
ã¯ãã¢ã³ã¢ãã¢äžã®ãªããŠã åã³ããåã¡ãã«ã«
ãã€ãŠåæã«è¡ãªããããããŠåŠçã¯å·åŽäžã«ã
ãã©ããããã©ã³äžã§è¡ãªãããã
ïŒäœçœ®ã®ã¢ã·ã«ãªãã·å®èœåºã¯ãšã¿ããŒã«äžã§
æ°Žé žåãããªãŠã ã«ãã€ãŠããåãããã
æ°Žé žåãããªãŠã ã«ãã€ãŠããåãããã
ïŒäœçœ®ã®ããããã·ã«å®èœåºã¯ãžããããã©ã³
ã«ãã€ãŠãããã¯ããããããŠåŠçã¯ããã©ãã
ããã©ã³äžã§ïœâãã«ãšã³ã¹ã«ãã³é žã®ååšäžã«
è¡ãªãããã
ã«ãã€ãŠãããã¯ããããããŠåŠçã¯ããã©ãã
ããã©ã³äžã§ïœâãã«ãšã³ã¹ã«ãã³é žã®ååšäžã«
è¡ãªãããã
21äœçœ®ã®ã¡ãã«åã¯ã«ãªãŠã ïœâããã©ãŒãã®
ååšäžã«ããåã¡ãã«ã«ãã€ãŠè¡ãªããããããŠ
åŠçã¯ãã«ãšã³äžã§è¡ãªãããã
ååšäžã«ããåã¡ãã«ã«ãã€ãŠè¡ãªããããããŠ
åŠçã¯ãã«ãšã³äžã§è¡ãªãããã
ïŒäœçœ®ã®ããããã·ã«å®èœåºãéé¢åãããé
ž
ã¯ãé ¢é žæ°Žæº¶æ¶²åã¯å¡©é žã®ãããªããã²ã³é žã§ã
ãã
ã¯ãé ¢é žæ°Žæº¶æ¶²åã¯å¡©é žã®ãããªããã²ã³é žã§ã
ãã
ïŒäœçœ®ã®ããããã·ã«å®èœåºããšãŒãã«åãã
ãããã«åãã¢ã«ãã«åºãçºçãããç©è³ªã¯ç¡«é ž
ãžã¡ãã«ã§ããããããŠåŠçã¯æ°Žé žåãããªãŠã
ã®ååšäžã«è¡ãªãããã
ãããã«åãã¢ã«ãã«åºãçºçãããç©è³ªã¯ç¡«é ž
ãžã¡ãã«ã§ããããããŠåŠçã¯æ°Žé žåãããªãŠã
ã®ååšäžã«è¡ãªãããã
æ¢ã«ç€ºããããã«ãäžè¬åŒã®ååç©ã¯ãããª
ããŠã æšèä»ãã¹ããã€ãèªå°äœã®åæçšã®åºçº
ç©è³ªã§ãããããããŠãæ¬çºæã®äž»é¡ããªããã®
åææ¹æ³ã¯ããæ°ŽçŽ ãé€ãå ã«èšèŒã®æå³ãæ
ããäžè¬åŒã®ååç©ã觊åªã®ååšäžã«ããªããŠ
ã åæ°ŽçŽ ãäœçšãããŠéå ããçæãããïŒïŒïŒ
â 3Hã17αïŒ21âãžã¡ãã«â19âãã«ãã¬ã°ã
âïŒïŒïŒïŒïŒ(10)âããªãšã³âïŒâROâ20âãªã³
ã«ããã¡ãã«åºãè¡šãããšãã¯ãããŒãåå¿ã«
ããã¢ã³ã¢ãã¢äžã®ãªããŠã ãçŽæ¥äœçšãããŠ
ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19âãã«ã
ã¬ã°ãâïŒïŒïŒ(10)âãžãšã³âïŒâã¡ããã·â20Ο
âãªãŒã«ãåŸããåã¯ããã¡ãã«åºä»¥å€ã®åºã
è¡šãããšãã¯ãé žãäœçšãããŠïŒäœçœ®ã®ãããã
ã·ã«å®èœåºãéé¢ãããç¡«é žãžã¡ãã«ãåå¿ã
ããçãããïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«
â19âãã«ãã¬ã°ãâïŒïŒïŒïŒïŒ(10)âããªãšã³â
ïŒâã¡ããã·â20âãªã³ã«ããŒãåå¿ã«ããã¢ã³
ã¢ãã¢äžã®ãªããŠã ãäœçšãããŠåæ§ã«ãïŒïŒïŒ
â 3Hã17αïŒ21âãžã¡ãã«â19âãã«ãã¬ã°ã
âïŒïŒïŒ(10)âãžãšã³âïŒâã¡ããã·â20ΟâãªãŒ
ã«ãåŸãããã«é ¢é žã®ãããªåŒ±é žæ°Žæº¶æ¶²ãåå¿ã
ããŠãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19â
ãã«ãã¬ã°ãâïŒ(10)âãšã³â20ΟâãªãŒã«âïŒâ
ãªã³ãåŸãããã«ããªãžããŠã ãã«ãããããäœ
çšãããçãããïŒïŒïŒâ 3Hã17αïŒ21âãžã¡
ãã«â19âãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³â20Ο
âãªãŒã«âïŒâãªã³ã«ã¯ãã ç¡«é žæ°Žæº¶æ¶²ãåå¿ã
ããŠææã®ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«
â19âãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20â
ãžãªã³ã圢æãããããšãç¹åŸŽãšããã
ããŠã æšèä»ãã¹ããã€ãèªå°äœã®åæçšã®åºçº
ç©è³ªã§ãããããããŠãæ¬çºæã®äž»é¡ããªããã®
åææ¹æ³ã¯ããæ°ŽçŽ ãé€ãå ã«èšèŒã®æå³ãæ
ããäžè¬åŒã®ååç©ã觊åªã®ååšäžã«ããªããŠ
ã åæ°ŽçŽ ãäœçšãããŠéå ããçæãããïŒïŒïŒ
â 3Hã17αïŒ21âãžã¡ãã«â19âãã«ãã¬ã°ã
âïŒïŒïŒïŒïŒ(10)âããªãšã³âïŒâROâ20âãªã³
ã«ããã¡ãã«åºãè¡šãããšãã¯ãããŒãåå¿ã«
ããã¢ã³ã¢ãã¢äžã®ãªããŠã ãçŽæ¥äœçšãããŠ
ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19âãã«ã
ã¬ã°ãâïŒïŒïŒ(10)âãžãšã³âïŒâã¡ããã·â20Ο
âãªãŒã«ãåŸããåã¯ããã¡ãã«åºä»¥å€ã®åºã
è¡šãããšãã¯ãé žãäœçšãããŠïŒäœçœ®ã®ãããã
ã·ã«å®èœåºãéé¢ãããç¡«é žãžã¡ãã«ãåå¿ã
ããçãããïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«
â19âãã«ãã¬ã°ãâïŒïŒïŒïŒïŒ(10)âããªãšã³â
ïŒâã¡ããã·â20âãªã³ã«ããŒãåå¿ã«ããã¢ã³
ã¢ãã¢äžã®ãªããŠã ãäœçšãããŠåæ§ã«ãïŒïŒïŒ
â 3Hã17αïŒ21âãžã¡ãã«â19âãã«ãã¬ã°ã
âïŒïŒïŒ(10)âãžãšã³âïŒâã¡ããã·â20ΟâãªãŒ
ã«ãåŸãããã«é ¢é žã®ãããªåŒ±é žæ°Žæº¶æ¶²ãåå¿ã
ããŠãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19â
ãã«ãã¬ã°ãâïŒ(10)âãšã³â20ΟâãªãŒã«âïŒâ
ãªã³ãåŸãããã«ããªãžããŠã ãã«ãããããäœ
çšãããçãããïŒïŒïŒâ 3Hã17αïŒ21âãžã¡
ãã«â19âãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³â20Ο
âãªãŒã«âïŒâãªã³ã«ã¯ãã ç¡«é žæ°Žæº¶æ¶²ãåå¿ã
ããŠææã®ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«
â19âãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20â
ãžãªã³ã圢æãããããšãç¹åŸŽãšããã
æ¬çºæã®åææ¹æ³ãå®æœããã®ã«å¿
èŠãªäžéäœ
ãšããŠã®äžèšã®ååç©ãããã
ãšããŠã®äžèšã®ååç©ãããã
ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19âã
ã«ãã¬ã°ãâïŒïŒïŒïŒïŒ(10)âããªãšã³âïŒâã¡ã
ãã·â20âãªã³ã ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19âã
ã«ãã¬ã°ãâïŒïŒïŒ(10)âãžãšã³âïŒâã¡ããã·â
20ΟâãªãŒã«ã ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19âã
ã«ãã¬ã°ãâïŒ(10)âãšã³â20ΟâãªãŒã«âïŒâãª
ã³åã³ ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19âã
ã«ãã¬ã°ãâïŒïŒïŒâãžãšã³â20ΟâãªãŒã«âïŒ
âãªã³ã
ã«ãã¬ã°ãâïŒïŒïŒïŒïŒ(10)âããªãšã³âïŒâã¡ã
ãã·â20âãªã³ã ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19âã
ã«ãã¬ã°ãâïŒïŒïŒ(10)âãžãšã³âïŒâã¡ããã·â
20ΟâãªãŒã«ã ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19âã
ã«ãã¬ã°ãâïŒ(10)âãšã³â20ΟâãªãŒã«âïŒâãª
ã³åã³ ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19âã
ã«ãã¬ã°ãâïŒïŒïŒâãžãšã³â20ΟâãªãŒã«âïŒ
âãªã³ã
ãããã®ååç©ã®äžã§ãããïŒïŒïŒâ 3Hã
17αïŒ21âãžã¡ãã«â19âãã«ãã¬ã°ãâïŒïŒïŒ
(10)âãžãšã³âïŒâã¡ããã·â20ΟâãªãŒã«ãç¹ã«
èå³ãããã
17αïŒ21âãžã¡ãã«â19âãã«ãã¬ã°ãâïŒïŒïŒ
(10)âãžãšã³âïŒâã¡ããã·â20ΟâãªãŒã«ãç¹ã«
èå³ãããã
ãããã®ååç©ã¯ãç¹ã«ã50CiïŒmMçšåºŠã®æ¯
æŸå°èœãæãããïŒïŒïŒâ 3Hã17αïŒ21âãžã¡
ãã«â19âãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ
20âãžãªã³ãå°ãã
æŸå°èœãæãããïŒïŒïŒâ 3Hã17αïŒ21âãžã¡
ãã«â19âãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ
20âãžãªã³ãå°ãã
ãã®åŸè
ã®ååç©ã¯ãåå®®ã·ããŸã«è¥ããã¯è
«
ç现èïŒåå®®çïŒã®ã·ã¯ããã©ãºã äžã®åã¯ã©ã
ãã«ãããŠDMBAïŒïŒïŒ10âãžã¡ãã«âïŒïŒïŒâ
ãã³ãŸã¢ã³ãã©ã»ã³ïŒã«ããèµ·ãããèªçºè «çäž
ã®ããã²ã¹ããã³ç¹ç°å容äœã容æã«æž¬å®ããã
ãã
ç现èïŒåå®®çïŒã®ã·ã¯ããã©ãºã äžã®åã¯ã©ã
ãã«ãããŠDMBAïŒïŒïŒ10âãžã¡ãã«âïŒïŒïŒâ
ãã³ãŸã¢ã³ãã©ã»ã³ïŒã«ããèµ·ãããèªçºè «çäž
ã®ããã²ã¹ããã³ç¹ç°å容äœã容æã«æž¬å®ããã
ãã
ãã®ååç©ã¯ãããã²ã¹ããã³ã®å Žåãšåãã
ãã«ãã©ã³ã¹ã³ã«ãã³ã«çµåããªããšããå©ç¹ã
æãããããã«ããã®ååç©ã¯ãäžèšããã²ã¹ã
ãã³ã®ç¹ç°å容äœã«å¯Ÿãã芪ååãåããã²ã¹ã
ãã³ã®èŠªåæ§ãããïŒãïŒå倧ããã
ãã«ãã©ã³ã¹ã³ã«ãã³ã«çµåããªããšããå©ç¹ã
æãããããã«ããã®ååç©ã¯ãäžèšããã²ã¹ã
ãã³ã®ç¹ç°å容äœã«å¯Ÿãã芪ååãåããã²ã¹ã
ãã³ã®èŠªåæ§ãããïŒãïŒå倧ããã
ããã²ã¹ããã³å容äœãç¹åŸŽã¥ããããã«
ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19âãã«ã
ã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãžãªã³ã䜿çš
ããããšã¯ãå€ãã®åè¡ç©ãäŸãã°ãJ.P.
RaynaudãD.Philibert äž¡æ°ãSteroidãJuly
1973ãP.89â97ã«èšèŒãããŠããã
ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19âãã«ã
ã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãžãªã³ã䜿çš
ããããšã¯ãå€ãã®åè¡ç©ãäŸãã°ãJ.P.
RaynaudãD.Philibert äž¡æ°ãSteroidãJuly
1973ãP.89â97ã«èšèŒãããŠããã
äžè¬åŒã®ååç©ã®è£œé æ³ã®åºçºç©è³ªã§ãããš
ã¹ãã©âïŒïŒïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâãª
ãŒã«â17âãªã³ã¯ãç±³åœç¹èš±ç¬¬2280828ã«èšèŒã
ããŠããã
ã¹ãã©âïŒïŒïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâãª
ãŒã«â17âãªã³ã¯ãç±³åœç¹èš±ç¬¬2280828ã«èšèŒã
ããŠããã
äžèšã®äŸã¯æ¬çºæãäŸç€ºãããã®ã§ããããå¶
éãããã®ã§ã¯ãªãã
éãããã®ã§ã¯ãªãã
äŸ ïŒïŒ17αïŒ21âãžã¡ãã«â19âãã«ãã¬ã°ã
âïŒïŒïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâã¡ãã
ã·â20âãªã³ å·¥çšïŒïŒ17αâãšããã«ãšã¹ãã©âïŒïŒïŒïŒïŒ
(10)ïŒïŒâããã©ãšã³âïŒïŒ17βâãžãªãŒã« çŽïŒïŒâã«å·åŽããã470c.c.ã®ããã©ãããã
ã©ã³ã®æº¶æ¶²ã«ã¢ã»ãã¬ã³ãå¹ã蟌ã¿ã23.5ïœã®ã«
ãªãŠã ïœâããã©ãŒãã次ãã§43c.c.ã®ãããµã¡ã
ã«ãã¹ãã«ããªã¢ãããå°å ¥ãããïŒïŒâã§40å
ãããŸãã11.75ïœã®ãšã¹ãã©âïŒïŒïŒïŒïŒ(10)ïŒ
ïŒâããã©ãšã³âïŒâãªãŒã«â17âãªã³ã350c.c.
ã®ããã©ããããã©ã³ã«æº¶è§£ããŠãªã溶液ãå ã
ããã¢ã»ãã¬ã³ããŸã å¹ã蟌ã¿ãªããåå¿æ··åç©
ãïŒïŒâã§ïŒæéãããŸãã次ãã§500c.c.ã®æ°Žã
å°å ¥ããé ¢é žãå ããŠPHïŒãïŒãšãããææ©çžã
ãã«ã³ããŒã·ãšã³ãããšãŒãã«ã§æœåºããæ°ŽæŽ
ããè±æ°Žãã掻æ§çã§åŠçããç空éããæžå§
äžã«æ¿çž®ä¹ŸåºãããïŒ3.9ïœã®ææååç©ãåŸãã
ãã¯ãã®ãŸãŸæ¬¡ã®å·¥çšã«çšããïŒå¡©åã¡ãã¬ã³ã
ãåçµæ¶ããããã®çæç©ã®è©Šæã¯ã178âã«ç
ããèç¹ãæãããïŒïŒãã®å·¥çšã®åºçºæã§çšãã
ãšã¹ãã©âïŒïŒïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâ
ãªãŒã«â17âãªã³ã¯ãç±³åœç¹èš±ç¬¬2280828å·ã«èš
èŒãããŠããã
âïŒïŒïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâã¡ãã
ã·â20âãªã³ å·¥çšïŒïŒ17αâãšããã«ãšã¹ãã©âïŒïŒïŒïŒïŒ
(10)ïŒïŒâããã©ãšã³âïŒïŒ17βâãžãªãŒã« çŽïŒïŒâã«å·åŽããã470c.c.ã®ããã©ãããã
ã©ã³ã®æº¶æ¶²ã«ã¢ã»ãã¬ã³ãå¹ã蟌ã¿ã23.5ïœã®ã«
ãªãŠã ïœâããã©ãŒãã次ãã§43c.c.ã®ãããµã¡ã
ã«ãã¹ãã«ããªã¢ãããå°å ¥ãããïŒïŒâã§40å
ãããŸãã11.75ïœã®ãšã¹ãã©âïŒïŒïŒïŒïŒ(10)ïŒ
ïŒâããã©ãšã³âïŒâãªãŒã«â17âãªã³ã350c.c.
ã®ããã©ããããã©ã³ã«æº¶è§£ããŠãªã溶液ãå ã
ããã¢ã»ãã¬ã³ããŸã å¹ã蟌ã¿ãªããåå¿æ··åç©
ãïŒïŒâã§ïŒæéãããŸãã次ãã§500c.c.ã®æ°Žã
å°å ¥ããé ¢é žãå ããŠPHïŒãïŒãšãããææ©çžã
ãã«ã³ããŒã·ãšã³ãããšãŒãã«ã§æœåºããæ°ŽæŽ
ããè±æ°Žãã掻æ§çã§åŠçããç空éããæžå§
äžã«æ¿çž®ä¹ŸåºãããïŒ3.9ïœã®ææååç©ãåŸãã
ãã¯ãã®ãŸãŸæ¬¡ã®å·¥çšã«çšããïŒå¡©åã¡ãã¬ã³ã
ãåçµæ¶ããããã®çæç©ã®è©Šæã¯ã178âã«ç
ããèç¹ãæãããïŒïŒãã®å·¥çšã®åºçºæã§çšãã
ãšã¹ãã©âïŒïŒïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâ
ãªãŒã«â17âãªã³ã¯ãç±³åœç¹èš±ç¬¬2280828å·ã«èš
èŒãããŠããã
å·¥çšïŒïŒ17αâãšããã«ãšã¹ãã©âïŒïŒïŒïŒïŒ
(10)ïŒïŒâããã©ãšã³âïŒïŒ17βâãžãªãŒã«ãžã¢
ã»ããŒã 13.9ïœã®å·¥çšïŒã§åŸãããååç©ã1.04ïœã®ïœ
âãã«ãšã³ã¹ã«ãã³é žãš33c.c.ã®ç¡æ°Žé ¢é žãšã®æ··å
ç©ãåšå²æž©åºŠã§ïŒæé30åãããŸãããç空é
ããé ¢é žã§æŽæµãã次ãã§æŽæµæ°Žãäžæ§ãšãªããŸ
ã§æ°ŽæŽãã也ç¥ããã11.1ïœã®ææååç©ãåŸ
ããMPïŒ189â190âã
(10)ïŒïŒâããã©ãšã³âïŒïŒ17βâãžãªãŒã«ãžã¢
ã»ããŒã 13.9ïœã®å·¥çšïŒã§åŸãããååç©ã1.04ïœã®ïœ
âãã«ãšã³ã¹ã«ãã³é žãš33c.c.ã®ç¡æ°Žé ¢é žãšã®æ··å
ç©ãåšå²æž©åºŠã§ïŒæé30åãããŸãããç空é
ããé ¢é žã§æŽæµãã次ãã§æŽæµæ°Žãäžæ§ãšãªããŸ
ã§æ°ŽæŽãã也ç¥ããã11.1ïœã®ææååç©ãåŸ
ããMPïŒ189â190âã
å·¥çšïŒïŒ17αâã¢ã»ãã«ãšã¹ãã©âïŒïŒïŒïŒïŒ
(10)ïŒïŒâããã©ãšã³âïŒïŒ17βâãžãªãŒã«ãžã¢
ã»ããŒã 11.05ïœã®å·¥çšïŒã§åŸãããååç©ã165c.c.ã®ãš
ã¿ããŒã«ã«å ããŠãªãæžæ¿ã«22ïœã®é ¢é žç¬¬äºæ°Žé
ã§æŽ»æ§åãããããŠãšãã¯ã¹50æš¹èïŒåŒ·é žåã€ãª
ã³äº€ææš¹èïŒãå ãã16æééæµãããã次ãã§
ç±éãããšã¿ããŒã«ã§æŽæµããæ¿çž®ä¹Ÿåºããã
åŸãããæ®çç©ã«44c.c.ã®ç¡æ°Žããªãžã³ãš22c.c.ã®ç¡
æ°Žé ¢é žãå ããåšå²æž©åºŠã§ïŒæéãããŸãããæ°·
æ°Žãå ããåŸãçµæ¶è³ªçæç©ãåŸãç空éãã
æ°ŽæŽãã80âã®ãªãŒãã³ã§ä¹Ÿç¥ããã10.92ïœã®
ææååç©ãååãããMPïŒ196âã
(10)ïŒïŒâããã©ãšã³âïŒïŒ17βâãžãªãŒã«ãžã¢
ã»ããŒã 11.05ïœã®å·¥çšïŒã§åŸãããååç©ã165c.c.ã®ãš
ã¿ããŒã«ã«å ããŠãªãæžæ¿ã«22ïœã®é ¢é žç¬¬äºæ°Žé
ã§æŽ»æ§åãããããŠãšãã¯ã¹50æš¹èïŒåŒ·é žåã€ãª
ã³äº€ææš¹èïŒãå ãã16æééæµãããã次ãã§
ç±éãããšã¿ããŒã«ã§æŽæµããæ¿çž®ä¹Ÿåºããã
åŸãããæ®çç©ã«44c.c.ã®ç¡æ°Žããªãžã³ãš22c.c.ã®ç¡
æ°Žé ¢é žãå ããåšå²æž©åºŠã§ïŒæéãããŸãããæ°·
æ°Žãå ããåŸãçµæ¶è³ªçæç©ãåŸãç空éãã
æ°ŽæŽãã80âã®ãªãŒãã³ã§ä¹Ÿç¥ããã10.92ïœã®
ææååç©ãååãããMPïŒ196âã
å·¥çšïŒïŒ17αâã¡ãã«â19âãã«ãã¬ã°ãâïŒïŒ
ïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâãªãŒã«â20â
ãªã³âã¢ã»ããŒã â70âã«å·åŽãã150c.c.ã®ã¢ã³ã¢ãã¢ãš570mgã®
ãªããŠã ãšã®æ··åç©ã15åéæ¥è§ŠãããŠããã次
ãã§150c.c.ã®ããã©ããããã©ã³ãå ããâ68âã«
å·åŽãã10.88ïœã®å·¥çšïŒã§åŸãããååç©ãå°
å ¥ããäžæŽ»æ§é°å²æ°äžã§ïŒæé45åãããŸããã
次ãã§ã10åéã«ããã€ãŠ44c.c.ã®ããåã¡ãã«ã
å ããåå¿æ··åç©ãâ69âã§ïŒæé30åä¿ã¡ãå
å¿æž©åºŠãïŒ15ã20âã«æ»ããåå¿æ··åç©ãæ°Žäžã«
泚ãããšãŒãã«ã§æœåºããäžæ§ã«ãªããŸã§æ°ŽæŽ
ããè±æ°Žããæžå§äžã«æ¿çž®ä¹ŸåºãããåŸãããæ®
çç©ãã·ãªã«ã§ã¯ãããã°ã©ãã€ãŒããé ¢é žãšã
ã«ãšãã³ãŒã³ãšã®æ··åç©ïŒïŒïŒïŒïŒã§æº¶é¢ããã
ããããŠãææååç©ãå«ã3.22ïœã®çµæ¶è³ªçæ
ç©ã®ç»åãååããããã®ç»åã«13c.c.ã®ããªãžã³
ãš6.5c.c.ã®ç¡æ°Žé ¢é žãå ããå¯å°å®¹åšäžã§ïŒæé
30åãããŸããæ°·ãå ããæ°Žã§åžéããç空é
ããæ°ŽæŽãã也ç¥ããããã®æ®çç©ãã·ãªã«ã§ã¯
ãããã°ã©ãã€ãŒãããšãŒãã«ãšç³æ²¹ãšãŒãã«
ïŒBPïŒ60â80âïŒãšã®æ··åç©ïŒïŒïŒïŒïŒã§æº¶é¢
ãã1.71ïœã®ææååç©ãåŸããMPïŒ140â142
âã
ïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâãªãŒã«â20â
ãªã³âã¢ã»ããŒã â70âã«å·åŽãã150c.c.ã®ã¢ã³ã¢ãã¢ãš570mgã®
ãªããŠã ãšã®æ··åç©ã15åéæ¥è§ŠãããŠããã次
ãã§150c.c.ã®ããã©ããããã©ã³ãå ããâ68âã«
å·åŽãã10.88ïœã®å·¥çšïŒã§åŸãããååç©ãå°
å ¥ããäžæŽ»æ§é°å²æ°äžã§ïŒæé45åãããŸããã
次ãã§ã10åéã«ããã€ãŠ44c.c.ã®ããåã¡ãã«ã
å ããåå¿æ··åç©ãâ69âã§ïŒæé30åä¿ã¡ãå
å¿æž©åºŠãïŒ15ã20âã«æ»ããåå¿æ··åç©ãæ°Žäžã«
泚ãããšãŒãã«ã§æœåºããäžæ§ã«ãªããŸã§æ°ŽæŽ
ããè±æ°Žããæžå§äžã«æ¿çž®ä¹ŸåºãããåŸãããæ®
çç©ãã·ãªã«ã§ã¯ãããã°ã©ãã€ãŒããé ¢é žãšã
ã«ãšãã³ãŒã³ãšã®æ··åç©ïŒïŒïŒïŒïŒã§æº¶é¢ããã
ããããŠãææååç©ãå«ã3.22ïœã®çµæ¶è³ªçæ
ç©ã®ç»åãååããããã®ç»åã«13c.c.ã®ããªãžã³
ãš6.5c.c.ã®ç¡æ°Žé ¢é žãå ããå¯å°å®¹åšäžã§ïŒæé
30åãããŸããæ°·ãå ããæ°Žã§åžéããç空é
ããæ°ŽæŽãã也ç¥ããããã®æ®çç©ãã·ãªã«ã§ã¯
ãããã°ã©ãã€ãŒãããšãŒãã«ãšç³æ²¹ãšãŒãã«
ïŒBPïŒ60â80âïŒãšã®æ··åç©ïŒïŒïŒïŒïŒã§æº¶é¢
ãã1.71ïœã®ææååç©ãåŸããMPïŒ140â142
âã
å·¥çšïŒïŒ17αâã¡ãã«â19âãã«ãã¬ã°ãâïŒïŒ
ïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâãªãŒã«â20â
ãªã³ 1.03ïœã®å·¥çšïŒ¡ã§åŸãããååç©ã20c.c.ã®ç¡æ°Ž
ãšã¿ããŒã«ãš2.9c.c.ã®1Næ°Žé žåãããªãŠã ã«å ã
ãŠãªãæžæ¿æ¶²ãäžæŽ»æ§é°å²æ°äžã«20âã§ïŒæéã
ããŸãããåå¿æ··åç©ãé ¢é žã®æ·»å ã«ããPHïŒïŒ
ãïŒãšãªããæ°Žã§åžéããç空éããæ°ŽæŽãã
也ç¥ããã805mgHgã®ææååç©ãåŸããMPïŒ
252âã
ïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâãªãŒã«â20â
ãªã³ 1.03ïœã®å·¥çšïŒ¡ã§åŸãããååç©ã20c.c.ã®ç¡æ°Ž
ãšã¿ããŒã«ãš2.9c.c.ã®1Næ°Žé žåãããªãŠã ã«å ã
ãŠãªãæžæ¿æ¶²ãäžæŽ»æ§é°å²æ°äžã«20âã§ïŒæéã
ããŸãããåå¿æ··åç©ãé ¢é žã®æ·»å ã«ããPHïŒïŒ
ãïŒãšãªããæ°Žã§åžéããç空éããæ°ŽæŽãã
也ç¥ããã805mgHgã®ææååç©ãåŸããMPïŒ
252âã
å·¥çšïŒïŒ17αâã¡ãã«â19âãã«ãã¬ã°ãâïŒïŒ
ïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâïŒÎ±âããã©
ããããã©ãã«ãªãã·ïŒâ20âãªã³ 0.8ïœã®å·¥çšïŒã§åŸãããååç©ã16c.c.ã®ãã
ã©ããããã©ã³ã0.8c.c.ã®ãžããããã©ã³åã³16
mgã®ïœâãã«ãšã³ã¹ã«ãã³é žã®æ··åç©ãäžæŽ»æ§é°
å²æ°äžã«20âã§ïŒæé30åãããŸããã次ãã§
0.4c.c.ã®ãžããããã©ã³ãå ãã20âã§ïŒæéä¿
ã¡ã10c.c.ã®éçé žãããªãŠã 飜å溶液ãå ããé ¢
é žãšãã«ã§æœåºããæ°ŽæŽããè±æ°Žããæ¿çž®ä¹Ÿåºã
ããåŸãããæ®çç©ãã·ãªã«ã§ã¯ãããã°ã©ãã€
ãŒãããã³ãŒã³ãšé ¢é žãšãã«ãšã®æ··åç©ïŒïŒïŒ
ïŒïŒã§æº¶é¢ããŠç²Ÿè£œãããïŒïœã®ææååç©ãå
åãããMP124âã
ïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâïŒÎ±âããã©
ããããã©ãã«ãªãã·ïŒâ20âãªã³ 0.8ïœã®å·¥çšïŒã§åŸãããååç©ã16c.c.ã®ãã
ã©ããããã©ã³ã0.8c.c.ã®ãžããããã©ã³åã³16
mgã®ïœâãã«ãšã³ã¹ã«ãã³é žã®æ··åç©ãäžæŽ»æ§é°
å²æ°äžã«20âã§ïŒæé30åãããŸããã次ãã§
0.4c.c.ã®ãžããããã©ã³ãå ãã20âã§ïŒæéä¿
ã¡ã10c.c.ã®éçé žãããªãŠã 飜å溶液ãå ããé ¢
é žãšãã«ã§æœåºããæ°ŽæŽããè±æ°Žããæ¿çž®ä¹Ÿåºã
ããåŸãããæ®çç©ãã·ãªã«ã§ã¯ãããã°ã©ãã€
ãŒãããã³ãŒã³ãšé ¢é žãšãã«ãšã®æ··åç©ïŒïŒïŒ
ïŒïŒã§æº¶é¢ããŠç²Ÿè£œãããïŒïœã®ææååç©ãå
åãããMP124âã
å·¥çšïŒïŒ17αïŒ21âãžã¡ãã«â19âãã«ãã¬ã°ã
âïŒïŒïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâïŒÎ±â
ããã©ããããã©ãã«ãªãã·ïŒâ20âãªã³ äžæŽ»æ§é°å²æ°äžã«740mgã®å·¥çšïŒã§åŸãããå
åç©ã7.5c.c.ã®ãã«ãšã³ã«æº¶è§£ãã次ãã§420mgã®
ã«ãªãŠã âïœâããã©ãŒããå ããããã®ããã«
åŸããã溶液ã20âã§15åãããŸãã0.475c.c.ã®
ããåã¡ãã«ãå ããåšå²æž©åºŠã§äžå€æŸçœ®ããã
æ°Žäžã«æ³šããé ¢é žãšãã«ã§æœåºããæŽæµæ°Žãäžæ§
ã«ãªããŸã§æ°ŽæŽããè±æ°Žããæžå§äžã«æ¿çž®ä¹Ÿåºã
ãããã®æ®çç©ãã·ãªã«ã§ã¯ãããã°ã©ãã€ãŒ
ãããã³ãŒã³ãšé ¢é žãšãã«ãšã®æ··åç©ïŒïŒïŒïŒïŒ
ã§æº¶é¢ããŠç²Ÿè£œããäºã€ã®ç»åãäžã€ã¯495mgã®
ææååç©ãå«æãããã®ãä»æ¹ã¯åºçºç©è³ªãšæ
æååç©ãšã®æ··åç©ãå«æãããã®ãåŸããåŸè
ã®ç»åãäžèšã®ããã«åŠçããåŸãåèšã§612mg
ã®ææååç©ãæš¹èç¶ç©ã®åœ¢ã§åŸããRfïŒ0.45ã
âïŒïŒïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâïŒÎ±â
ããã©ããããã©ãã«ãªãã·ïŒâ20âãªã³ äžæŽ»æ§é°å²æ°äžã«740mgã®å·¥çšïŒã§åŸãããå
åç©ã7.5c.c.ã®ãã«ãšã³ã«æº¶è§£ãã次ãã§420mgã®
ã«ãªãŠã âïœâããã©ãŒããå ããããã®ããã«
åŸããã溶液ã20âã§15åãããŸãã0.475c.c.ã®
ããåã¡ãã«ãå ããåšå²æž©åºŠã§äžå€æŸçœ®ããã
æ°Žäžã«æ³šããé ¢é žãšãã«ã§æœåºããæŽæµæ°Žãäžæ§
ã«ãªããŸã§æ°ŽæŽããè±æ°Žããæžå§äžã«æ¿çž®ä¹Ÿåºã
ãããã®æ®çç©ãã·ãªã«ã§ã¯ãããã°ã©ãã€ãŒ
ãããã³ãŒã³ãšé ¢é žãšãã«ãšã®æ··åç©ïŒïŒïŒïŒïŒ
ã§æº¶é¢ããŠç²Ÿè£œããäºã€ã®ç»åãäžã€ã¯495mgã®
ææååç©ãå«æãããã®ãä»æ¹ã¯åºçºç©è³ªãšæ
æååç©ãšã®æ··åç©ãå«æãããã®ãåŸããåŸè
ã®ç»åãäžèšã®ããã«åŠçããåŸãåèšã§612mg
ã®ææååç©ãæš¹èç¶ç©ã®åœ¢ã§åŸããRfïŒ0.45ã
å·¥çšïŒïŒ17αïŒ21âãžã¡ãã«â19âãã«ãã¬ã°ã
âïŒïŒïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâãªãŒã«
â20âãªã³ 0.57ïœã®å·¥çšïŒã§åŸãããååç©ã20ïŒ ã®æ°Žã
å«æãã5.8c.c.ã®é ¢é žã«æº¶è§£ããŠãªã溶液ã50â
ã§ïŒæéãããŸããã次ãã§åå¿æ··åç©ãæ°Žäžã«
泚ããå¡©åã¡ãã¬ã³ã§æœåºããæ°ŽæŽããè±æ°Žãã
æžå§äžã«æ¿çž®ä¹Ÿåºããããã®æ®çç©ããã³ãŒã³ãš
é ¢é žãšãã«ãšã®æ··åç©ïŒïŒïŒïŒïŒã次ãã§ãšãŒã
ã«ãšç³æ²¹ãšãŒãã«ïŒBPïŒ60ã80âïŒã溶é¢æ¶²ãš
ããŠã·ãªã«ã§ïŒåã¯ãããã°ã©ãã€ãŒããåŸã73
mgã®ææååç©ãåŸããMPïŒ209âã
âïŒïŒïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâãªãŒã«
â20âãªã³ 0.57ïœã®å·¥çšïŒã§åŸãããååç©ã20ïŒ ã®æ°Žã
å«æãã5.8c.c.ã®é ¢é žã«æº¶è§£ããŠãªã溶液ã50â
ã§ïŒæéãããŸããã次ãã§åå¿æ··åç©ãæ°Žäžã«
泚ããå¡©åã¡ãã¬ã³ã§æœåºããæ°ŽæŽããè±æ°Žãã
æžå§äžã«æ¿çž®ä¹Ÿåºããããã®æ®çç©ããã³ãŒã³ãš
é ¢é žãšãã«ãšã®æ··åç©ïŒïŒïŒïŒïŒã次ãã§ãšãŒã
ã«ãšç³æ²¹ãšãŒãã«ïŒBPïŒ60ã80âïŒã溶é¢æ¶²ãš
ããŠã·ãªã«ã§ïŒåã¯ãããã°ã©ãã€ãŒããåŸã73
mgã®ææååç©ãåŸããMPïŒ209âã
åæïŒC22H28O2
èšç®ïŒïŒ£ïŒ
81.45 ïŒ
8.70
å®æž¬ïŒ 80.9 8.7
å·¥çšïŒïŒ17αïŒ21âãžã¡ãã«â19âãã«ãã¬ã°ã
âïŒïŒïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâã¡ããã·
â20âãªã³ 50mgã®å·¥çšïŒã§åŸãããååç©ãïŒc.c.ã®ã¢ã»ã
ã³åã³ïŒc.c.ã®2Næ°Žé žåãããªãŠã ã®æ··åç©ãé
æµããã0.5c.c.ã®ç¡«é žãžã¡ãã«ãšïŒc.c.ã®2Næ°Žé žå
ãããªãŠã ãå ããã10åéæŸçœ®ããåå¿æ··åç©
ã«0.5c.c.ã®ç¡«é žãžã¡ãã«ãšïŒc.c.ã®2Næ°Žé žåãããª
ãŠã ãå ããããã®æº¶æ¶²ã10åéãããŸãã10c.c.
ã®æ°Žã泚ãããã³ãŒã³ã§æœåºããæ°ŽæŽããè±æ°Ž
ããèžçºä¹Ÿåºããã57mgã®ææååç©ãçµæ¶åœ¢ãš
ããŠåŸãïŒãã³ãŒã³ãšé ¢é žãšãã«ãšã®æ··åç©
ïŒïŒïŒïŒïŒã溶é¢æ¶²ãšããŠã·ãªã«ã§ã¯ãããã°ã©
ãã€ãŒãRfïŒ0.7ïŒã
âïŒïŒïŒïŒïŒ(10)ïŒïŒâããã©ãšã³âïŒâã¡ããã·
â20âãªã³ 50mgã®å·¥çšïŒã§åŸãããååç©ãïŒc.c.ã®ã¢ã»ã
ã³åã³ïŒc.c.ã®2Næ°Žé žåãããªãŠã ã®æ··åç©ãé
æµããã0.5c.c.ã®ç¡«é žãžã¡ãã«ãšïŒc.c.ã®2Næ°Žé žå
ãããªãŠã ãå ããã10åéæŸçœ®ããåå¿æ··åç©
ã«0.5c.c.ã®ç¡«é žãžã¡ãã«ãšïŒc.c.ã®2Næ°Žé žåãããª
ãŠã ãå ããããã®æº¶æ¶²ã10åéãããŸãã10c.c.
ã®æ°Žã泚ãããã³ãŒã³ã§æœåºããæ°ŽæŽããè±æ°Ž
ããèžçºä¹Ÿåºããã57mgã®ææååç©ãçµæ¶åœ¢ãš
ããŠåŸãïŒãã³ãŒã³ãšé ¢é žãšãã«ãšã®æ··åç©
ïŒïŒïŒïŒïŒã溶é¢æ¶²ãšããŠã·ãªã«ã§ã¯ãããã°ã©
ãã€ãŒãRfïŒ0.7ïŒã
äŸ ïŒïŒãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19
âãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãž
ãªã³ å·¥çšïŒ¡ïŒãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19
âãã«ãã¬ã°ãâïŒïŒïŒïŒïŒ(10)âããªãšã³âïŒ
âã¡ããã·â20âãªã³ 10mgã®ãã©ãžãŠã æ æçã57mgã®17αïŒ21âãž
ã¡ãã«â19âãã«ãã¬ã°ãâïŒïŒïŒïŒïŒ(10)ïŒïŒâ
ããã©ãšã³âïŒâã¡ããã·â20âãªã³åã³1.5ml
ã®é ¢é žãšãã«ãããªãåå¿æ··åç©ã液äœçªçŽ ã§å·
åŽãã次ãã§ïŒâåžžå§äžã§ç空äžã«2950ïœCiïŒc.c.
ã®æ¯æŸå°èœãæãã3.86c.c.ã®ããªããŠã ãå°å ¥ã
ãã次ãã§ãã®åå¿æ··åç©ãåšå²æž©åºŠã«æ»ããïŒ
æéãããŸãç¶ããéå°ã®ããªããŠã ãååãã
éãã溶åªãæžå§äžã«çå»ããäžèŠããªããŠã
ãé€å»ããåŸã51CiïŒïœã¢ã«ã®æ¯æŸå°èœãæãã
44mgã®ææã®ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ã
ã«â19âãã«ãã¬ã°ãâïŒïŒïŒïŒïŒ(10)âããªãšã³
âïŒâã¡ããã·â20âãªã³ãåŸãã
âãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãž
ãªã³ å·¥çšïŒ¡ïŒãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19
âãã«ãã¬ã°ãâïŒïŒïŒïŒïŒ(10)âããªãšã³âïŒ
âã¡ããã·â20âãªã³ 10mgã®ãã©ãžãŠã æ æçã57mgã®17αïŒ21âãž
ã¡ãã«â19âãã«ãã¬ã°ãâïŒïŒïŒïŒïŒ(10)ïŒïŒâ
ããã©ãšã³âïŒâã¡ããã·â20âãªã³åã³1.5ml
ã®é ¢é žãšãã«ãããªãåå¿æ··åç©ã液äœçªçŽ ã§å·
åŽãã次ãã§ïŒâåžžå§äžã§ç空äžã«2950ïœCiïŒc.c.
ã®æ¯æŸå°èœãæãã3.86c.c.ã®ããªããŠã ãå°å ¥ã
ãã次ãã§ãã®åå¿æ··åç©ãåšå²æž©åºŠã«æ»ããïŒ
æéãããŸãç¶ããéå°ã®ããªããŠã ãååãã
éãã溶åªãæžå§äžã«çå»ããäžèŠããªããŠã
ãé€å»ããåŸã51CiïŒïœã¢ã«ã®æ¯æŸå°èœãæãã
44mgã®ææã®ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ã
ã«â19âãã«ãã¬ã°ãâïŒïŒïŒïŒïŒ(10)âããªãšã³
âïŒâã¡ããã·â20âãªã³ãåŸãã
å·¥çšïŒ¢ïŒãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19
âãã«ãã¬ã°ãâïŒïŒïŒïŒ(10)âãžãšã³âïŒâã¡
ããã·â20ΟâãªãŒã« â35âãâ40âã®éã«å·åŽãã25c.c.ã®ã¢ã³ã¢ã
ã¢ã«44mgã®ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«
â19âãã«ãã¬ã°ãâïŒïŒïŒïŒïŒ(10)âããªãšã³â
ïŒâã¡ããã·â20âãªã³ãïŒc.c.ã®ããã©ãããã
ã©ã³ã0.5c.c.ã®ãšã¿ããŒã«åã³200mgã®ãªããŠã ã
å ããããã®åå¿æ··åç©ãâ35âã§ïŒæéãããŸ
ãç¶ãã次ãã§10åéã«ããã10c.c.ã®ãšã¿ããŒã«
ãå ãã次ãã§åšå²æž©åºŠã«æ»ãããšã«ããã¢ã³ã¢
ãã¢ãé€å»ããå¡©åã¡ãã¬ã³ã§æ°åæœåºããç¡«é ž
ãããªãŠã ã§è±æ°Žããæžå§äžã«èžçºããã48mgã®
ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19âãã«ã
ã¬ã°ãâïŒïŒïŒ(10)âãžãšã³âïŒâã¡ããã·â20Ο
âãªãŒã«ãæš¹èç¶ç©ãšããŠåŸãããã¯ãã®ãŸãŸæ¬¡
ã®åæå·¥çšã«çšããã
âãã«ãã¬ã°ãâïŒïŒïŒïŒ(10)âãžãšã³âïŒâã¡
ããã·â20ΟâãªãŒã« â35âãâ40âã®éã«å·åŽãã25c.c.ã®ã¢ã³ã¢ã
ã¢ã«44mgã®ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«
â19âãã«ãã¬ã°ãâïŒïŒïŒïŒïŒ(10)âããªãšã³â
ïŒâã¡ããã·â20âãªã³ãïŒc.c.ã®ããã©ãããã
ã©ã³ã0.5c.c.ã®ãšã¿ããŒã«åã³200mgã®ãªããŠã ã
å ããããã®åå¿æ··åç©ãâ35âã§ïŒæéãããŸ
ãç¶ãã次ãã§10åéã«ããã10c.c.ã®ãšã¿ããŒã«
ãå ãã次ãã§åšå²æž©åºŠã«æ»ãããšã«ããã¢ã³ã¢
ãã¢ãé€å»ããå¡©åã¡ãã¬ã³ã§æ°åæœåºããç¡«é ž
ãããªãŠã ã§è±æ°Žããæžå§äžã«èžçºããã48mgã®
ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19âãã«ã
ã¬ã°ãâïŒïŒïŒ(10)âãžãšã³âïŒâã¡ããã·â20Ο
âãªãŒã«ãæš¹èç¶ç©ãšããŠåŸãããã¯ãã®ãŸãŸæ¬¡
ã®åæå·¥çšã«çšããã
å·¥çšïŒ£ïŒãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19
âãã«ãã¬ã°ãâïŒ(10)âãšã³â20ΟâãªãŒã«â
ïŒâãªã³ 25ïŒ ã®æ°Žãå«æããïŒc.c.ã®é ¢é žã«ãäžæŽ»æ§ã¬ã¹
ãå¹ã蟌ã¿äžã€ãããŸããªããã48mgã®ãïŒïŒïŒ
â 3Hã17αïŒ21âãžã¡ãã«â19âãã«ãã¬ã°ã
âïŒïŒïŒ(10)ãžãšã³âïŒâã¡ããã·â20ΟâãªãŒã«
ãå°å ¥ãããïŒæéãããŸãç¶ãã次ãã§æ°Žãæ°
åå ããçæç©ãç空éãããããæ°Žãé žæ§ç
é žãããªãŠã 飜å溶液ã次ãã§æ°Žã§é 次æŽæµãã
æžå§äžã«ä¹Ÿç¥ããçæç©ãå¡©åã¡ãã¬ã³ãšã€ãœã
ããã«ãšãŒãã«ãšã®æ··åç©ããåçµæ¶ããŠç²Ÿè£œã
ãã50mgã®ææååç©ãåŸãã
âãã«ãã¬ã°ãâïŒ(10)âãšã³â20ΟâãªãŒã«â
ïŒâãªã³ 25ïŒ ã®æ°Žãå«æããïŒc.c.ã®é ¢é žã«ãäžæŽ»æ§ã¬ã¹
ãå¹ã蟌ã¿äžã€ãããŸããªããã48mgã®ãïŒïŒïŒ
â 3Hã17αïŒ21âãžã¡ãã«â19âãã«ãã¬ã°ã
âïŒïŒïŒ(10)ãžãšã³âïŒâã¡ããã·â20ΟâãªãŒã«
ãå°å ¥ãããïŒæéãããŸãç¶ãã次ãã§æ°Žãæ°
åå ããçæç©ãç空éãããããæ°Žãé žæ§ç
é žãããªãŠã 飜å溶液ã次ãã§æ°Žã§é 次æŽæµãã
æžå§äžã«ä¹Ÿç¥ããçæç©ãå¡©åã¡ãã¬ã³ãšã€ãœã
ããã«ãšãŒãã«ãšã®æ··åç©ããåçµæ¶ããŠç²Ÿè£œã
ãã50mgã®ææååç©ãåŸãã
å·¥çšïŒ€ïŒãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19
âãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³â20ΟâãªãŒ
ã«âïŒâãªã³ åšå²æž©åºŠã§ãããŸããªããã0.5c.c.ã®ããªãžã³
ã«50mgã®ãïŒïŒïŒâ +Hã17αïŒ21âãžã¡ãã«â
19âãã«ãã¬ã°ãâïŒ(10)âãšã³â20ΟâãªãŒã«â
ïŒâãªã³ãå°å ¥ããã次ãã§çŽâ14âã«å·åŽãã
45åéã«ããã€ãŠ35mgã®ããªãžããŠã ãã«ããã
ããå°å ¥ãããåå¿æ··åç©ãäžèšæž©åºŠã§45åéä¿
ã¡ã次ãã§æž©åºŠãåã³çŽ20âã«äžæããããææ
ã§äžã€åšå²æž©åºŠã§18æéãããŸãç¶ããæ°Žãæ°·å
ã³å¡©é žã®æ··åç©ïŒïŒïŒïŒïŒïŒïŒã«æ³šå ¥ãã45åã
ããŸããç空éããäžæ§ã«ãªããŸã§æ°ŽæŽãã也
ç¥ãã52mgã®ææååç©ãåŸãããã®ååç©ã¯ã
ãã®ãŸãŸæ¬¡ã®åæå·¥çšã«çšããããšãã§ããã
âãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³â20ΟâãªãŒ
ã«âïŒâãªã³ åšå²æž©åºŠã§ãããŸããªããã0.5c.c.ã®ããªãžã³
ã«50mgã®ãïŒïŒïŒâ +Hã17αïŒ21âãžã¡ãã«â
19âãã«ãã¬ã°ãâïŒ(10)âãšã³â20ΟâãªãŒã«â
ïŒâãªã³ãå°å ¥ããã次ãã§çŽâ14âã«å·åŽãã
45åéã«ããã€ãŠ35mgã®ããªãžããŠã ãã«ããã
ããå°å ¥ãããåå¿æ··åç©ãäžèšæž©åºŠã§45åéä¿
ã¡ã次ãã§æž©åºŠãåã³çŽ20âã«äžæããããææ
ã§äžã€åšå²æž©åºŠã§18æéãããŸãç¶ããæ°Žãæ°·å
ã³å¡©é žã®æ··åç©ïŒïŒïŒïŒïŒïŒïŒã«æ³šå ¥ãã45åã
ããŸããç空éããäžæ§ã«ãªããŸã§æ°ŽæŽãã也
ç¥ãã52mgã®ææååç©ãåŸãããã®ååç©ã¯ã
ãã®ãŸãŸæ¬¡ã®åæå·¥çšã«çšããããšãã§ããã
å·¥çšïŒ¥ïŒãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19
âãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãž
ãªã³ 52mgã®ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â
19âãã«ãã¬ã°ãâïŒïŒïŒ(10)âãžãšã³â20Οâãª
ãŒã«âïŒâãªã³ãïŒc.c.ã®ã¢ã»ãã³ã«ãããŸããªã
ãå°å ¥ãããå®å šã«æº¶è§£ããåŸã25âãè¶ ããªã
枩床ã§ã5.1ïœã®ç¡æ°Žã¯ãã é žã4.6c.c.ã®ç¡«é žåã³
20c.c.ã®æ°Žãå«æãã0.01c.c.ã®ã¯ãã ç¡«é žæº¶æ¶²ãå
ããããã®æäœãïŒå以äžç¹°ãè¿ããçããåå¿
æ··åç©ã«æ°åæ°Žãå ãã35â以äžã®æž©åºŠã§æžå§èž
çãã次ãã§æžå§äžã«20âã«å·åŽãããç空é
ãããã®æ®çç©ãäžæ§ãšãªããŸã§æŽæµãã50mgã®
çæç©ãåŸããããèå±€ã¯ãããã°ã©ãã€ãŒïŒã
ã³ãŒã³ãšé ¢é žãšãã«85ïŒ15ïŒã§ç²Ÿè£œããŠïŒmgã®æ
æååç©ãåŸãããã®æ¯æŸå°èœã¯51.4CiïŒmMã§
ãã€ãã
âãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãž
ãªã³ 52mgã®ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â
19âãã«ãã¬ã°ãâïŒïŒïŒ(10)âãžãšã³â20Οâãª
ãŒã«âïŒâãªã³ãïŒc.c.ã®ã¢ã»ãã³ã«ãããŸããªã
ãå°å ¥ãããå®å šã«æº¶è§£ããåŸã25âãè¶ ããªã
枩床ã§ã5.1ïœã®ç¡æ°Žã¯ãã é žã4.6c.c.ã®ç¡«é žåã³
20c.c.ã®æ°Žãå«æãã0.01c.c.ã®ã¯ãã ç¡«é žæº¶æ¶²ãå
ããããã®æäœãïŒå以äžç¹°ãè¿ããçããåå¿
æ··åç©ã«æ°åæ°Žãå ãã35â以äžã®æž©åºŠã§æžå§èž
çãã次ãã§æžå§äžã«20âã«å·åŽãããç空é
ãããã®æ®çç©ãäžæ§ãšãªããŸã§æŽæµãã50mgã®
çæç©ãåŸããããèå±€ã¯ãããã°ã©ãã€ãŒïŒã
ã³ãŒã³ãšé ¢é žãšãã«85ïŒ15ïŒã§ç²Ÿè£œããŠïŒmgã®æ
æååç©ãåŸãããã®æ¯æŸå°èœã¯51.4CiïŒmMã§
ãã€ãã
Claims (1)
- ãç¹èš±è«æ±ã®ç¯å²ã ïŒ æ¬¡ã®äžè¬åŒ ïŒããã§ïŒ²ã¯ïŒãïŒåã®ççŽ ååãå«æããã¢ã«
ãã«åºåã¯ããã©ããããã©ãã«ãããªãã«è¥ã
ãã¯ããªã¡ãã«ã·ãªã«åºãè¡šããïŒ ã®ã¹ããã€ãã觊åªã®ååšäžã«ããªããŠã åæ°ŽçŽ
ãäœçšãããŠéå ããçæãããïŒïŒïŒâ 3Hã
17αïŒ21âãžã¡ãã«â19âãã«ãã¬ã°ãâïŒïŒ
ïŒïŒïŒ(10)âããªãšã³âïŒâROâ20âãªã³ã«ã
ãã¡ãã«åºãè¡šãããšãã¯ãã¢ã³ã¢ãã¢äžã®ãªã
ãŠã ãçŽæ¥äœçšãããŠãïŒïŒïŒâ 3Hã17αïŒ21
âãžã¡ãã«â19âãã«ãã¬ã°ãâïŒïŒïŒ(10)âãžãš
ã³âïŒâã¡ããã·â20ΟâãªãŒã«ãåŸããåã¯ã
ãã¡ãã«åºä»¥å€ã®åèšã®åºãè¡šãããšãã¯ãé ž
ãäœçšãããŠïŒäœçœ®ã®ããããã·ã«å®èœåºãéé¢
ãããç¡«é žãžã¡ãã«ãåå¿ãããçãããïŒïŒïŒ
â 3Hã17αïŒ21âãžã¡ãã«â19âãã«ãã¬ã°ã
âïŒïŒïŒïŒïŒ(10)âããªãšã³âïŒâã¡ããã·â20â
ãªã³ã«ã¢ã³ã¢ãã¢äžã®ãªããŠã ãäœçšãããŠåæ§
ã«ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19âã
ã«ãã¬ã°ãâïŒïŒïŒ(10)âãžãšã³âïŒâã¡ããã·â
20ΟâãªãŒã«ãåŸãããã«åŒ±é žæ°Žæº¶æ¶²ãäœçšãã
ãŠãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â19âã
ã«ãã¬ã°ãâïŒ(10)âãšã³â20ΟâãªãŒã«âïŒâãª
ã³ãåŸãããã«ããªãžããŠã ãã«ãããããäœçš
ãããçãããïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ã
ã«â19âãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³â20Οâ
ãªãŒã«âïŒâãªã³ã«ã¯ãã ç¡«é žæ°Žæº¶æ¶²ãåå¿ãã
ãŠææã®ãïŒïŒïŒâ 3Hã17αïŒ21âãžã¡ãã«â
19âãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãž
ãªã³ã圢æãããããšãç¹åŸŽãšããããªããŠã æš
èä»ãã¹ããã€ãã®åææ¹æ³ã
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR76-37623 | 1976-12-14 | ||
| FR7637623A FR2374335A1 (fr) | 1976-12-14 | 1976-12-14 | Nouveaux steroides, leur procede de preparation et leur application dans la synthese de steroides marques au tritium |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS61225195A JPS61225195A (ja) | 1986-10-06 |
| JPS6360038B2 true JPS6360038B2 (ja) | 1988-11-22 |
Family
ID=9181041
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP14890477A Granted JPS5373553A (en) | 1976-12-14 | 1977-12-13 | Novel steroid process for preparing same and method of using same for synthesizing tritium labelled steroid |
| JP61016008A Granted JPS61225195A (ja) | 1976-12-14 | 1986-01-29 | ããªããŠã æšèä»ãã¹ããã€ãã®åæ |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP14890477A Granted JPS5373553A (en) | 1976-12-14 | 1977-12-13 | Novel steroid process for preparing same and method of using same for synthesizing tritium labelled steroid |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US4152325A (ja) |
| JP (2) | JPS5373553A (ja) |
| CH (1) | CH626378A5 (ja) |
| DE (1) | DE2755818A1 (ja) |
| FR (1) | FR2374335A1 (ja) |
| GB (1) | GB1578900A (ja) |
| NL (1) | NL7713768A (ja) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2430953A1 (fr) * | 1978-07-13 | 1980-02-08 | Roussel Uclaf | Nouveaux derives 3,20-dioxo 4,9-diene 21-hydroxyle, leur procede de preparation et leur application comme medicaments |
| US7910755B2 (en) * | 2004-09-29 | 2011-03-22 | Harbor Biosciences, Inc. | Stem cell expansion and uses |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB853012A (en) * | 1958-06-26 | 1960-11-02 | British Drug Houses Ltd | 1:6-dimethyl aromatic steroids and the preparation thereof |
| NL124323C (ja) * | 1963-03-27 | |||
| FR2077877B1 (ja) * | 1970-02-20 | 1974-02-01 | Roussel Uclaf | |
| US3709878A (en) * | 1970-07-20 | 1973-01-09 | Sandoz Ag | 8 alpha-methyl-substituted-steroids |
| FR2149302A1 (en) * | 1971-08-19 | 1973-03-30 | Roussel Uclaf | 21-methyl pregnadienes prepn - used as progestomimetics |
-
1976
- 1976-12-14 FR FR7637623A patent/FR2374335A1/fr active Granted
-
1977
- 1977-11-28 US US05/855,177 patent/US4152325A/en not_active Expired - Lifetime
- 1977-12-13 JP JP14890477A patent/JPS5373553A/ja active Granted
- 1977-12-13 NL NL7713768A patent/NL7713768A/xx not_active Application Discontinuation
- 1977-12-14 GB GB51969/77A patent/GB1578900A/en not_active Expired
- 1977-12-14 CH CH1538977A patent/CH626378A5/fr not_active IP Right Cessation
- 1977-12-14 DE DE19772755818 patent/DE2755818A1/de not_active Ceased
-
1986
- 1986-01-29 JP JP61016008A patent/JPS61225195A/ja active Granted
Also Published As
| Publication number | Publication date |
|---|---|
| JPS61225195A (ja) | 1986-10-06 |
| FR2374335A1 (fr) | 1978-07-13 |
| JPS5373553A (en) | 1978-06-30 |
| GB1578900A (en) | 1980-11-12 |
| DE2755818A1 (de) | 1978-06-15 |
| FR2374335B1 (ja) | 1979-03-30 |
| JPS6126797B2 (ja) | 1986-06-21 |
| CH626378A5 (ja) | 1981-11-13 |
| US4152325A (en) | 1979-05-01 |
| NL7713768A (nl) | 1978-06-16 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JPH0369919B2 (ja) | ||
| FR2569408A1 (fr) | Nouveaux steroides substitues en position 10 par un radical comportant une double ou triple liaison, leur procede de preparation, leur application comme medicaments, les compositions pharmaceutiques les renfermant | |
| JPS6360038B2 (ja) | ||
| CA1260929A (en) | Process for the preparation of pregnane derivatives | |
| JPH0320399B2 (ja) | ||
| JPH0480038B2 (ja) | ||
| JP2509467B2 (ja) | ïŒâã¢ã«ã³ãã·âïŒïŒâã¡ãã«âïŒïŒïŒâãšã¹ãã©ãžãšã³âïŒïŒâãªã³ | |
| JPS6360035B2 (ja) | ||
| JPH036158B2 (ja) | ||
| US4031074A (en) | Process for the preparation of 11β-hydroxy-18-alkyl-estrane compounds | |
| JPS641480B2 (ja) | ||
| US4585591A (en) | 17β-ethynylsteroids and process for preparing same | |
| JP4361976B2 (ja) | ãšã¹ããã²ã³æ··åç©ã®ç¡«é žå | |
| US2744110A (en) | 3-ethylene mercaptole derivatives of progesterone | |
| US3324152A (en) | 1alpha-methyl-delta2-androstenes | |
| US4165326A (en) | Steroids and their preparation | |
| JPS6210238B2 (ja) | ||
| JPS6044317B2 (ja) | ïŒïŒÎ²âããããã·âïŒïŒâã¢ã«ãã«âãšã¹ãã©ã³ååç©ã®è£œæ³ | |
| US3405128A (en) | 18-alkylated-17alpha-(2-alkynyl)estra-1, 3, 5(10)-triene-3, 17beta-diols, ethers andesters thereof | |
| JPS5970700A (ja) | ïŒÎ±âã¢ã«ãã«âïŒïŒÎ±âãã¬ã°ã³âïŒâãšã³âïŒïŒïŒïŒïŒâã«ã«ãã©ã¯ãã³åã³âïŒïŒâã«ã«ãã³é žå¡©ããã®è£œæ³äžŠã³ã«è©²ååç©ãå«æããæã¢ã«ãã¹ããã³äœçšãæãã補è¬çè£œå€ | |
| US3998813A (en) | Process for the preparation of 11β-hydroxy-18-alkyl-estrane compounds | |
| US3274183A (en) | 3-(17beta-hydroxy-1, 4-dimethylestra-1, 3, 5(10)-trien-17alpha-yl) propionic acid lactone and intermediates | |
| Popova et al. | Synthesis of pregnane derivatives | |
| JPS6214556B2 (ja) | ||
| CH629504A5 (en) | 19-Norpregnatetraene derivatives |