HRP20140373T2 - Postupak proizvodnje kiralnih 8-(3-amino-piperidin-1-il)-ksantina - Google Patents
Postupak proizvodnje kiralnih 8-(3-amino-piperidin-1-il)-ksantina Download PDFInfo
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- HRP20140373T2 HRP20140373T2 HRP20140373TT HRP20140373T HRP20140373T2 HR P20140373 T2 HRP20140373 T2 HR P20140373T2 HR P20140373T T HRP20140373T T HR P20140373TT HR P20140373 T HRP20140373 T HR P20140373T HR P20140373 T2 HRP20140373 T2 HR P20140373T2
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- 238000000034 method Methods 0.000 title claims 21
- 238000004519 manufacturing process Methods 0.000 title claims 11
- WNHHLYZOSOUUQW-UHFFFAOYSA-N 8-(3-aminopiperidin-1-yl)-3,7-dihydropurine-2,6-dione Chemical class C1C(N)CCCN1C(N1)=NC2=C1C(=O)NC(=O)N2 WNHHLYZOSOUUQW-UHFFFAOYSA-N 0.000 title 1
- -1 phenylcarbonylmethyl Chemical group 0.000 claims 21
- 150000001875 compounds Chemical class 0.000 claims 15
- 239000003814 drug Substances 0.000 claims 15
- 229940079593 drug Drugs 0.000 claims 12
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 10
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 6
- 239000000969 carrier Substances 0.000 claims 5
- 239000003085 diluting agent Substances 0.000 claims 5
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 claims 3
- 238000006243 chemical reaction Methods 0.000 claims 3
- 238000002425 crystallisation Methods 0.000 claims 3
- 230000008025 crystallization Effects 0.000 claims 3
- 238000010511 deprotection reaction Methods 0.000 claims 3
- HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 claims 2
- POAZMSVKCTYEPJ-SECBINFHSA-N 2-[(3r)-piperidin-3-yl]isoindole-1,3-dione Chemical compound O=C1C2=CC=CC=C2C(=O)N1[C@@H]1CCCNC1 POAZMSVKCTYEPJ-SECBINFHSA-N 0.000 claims 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- NLKBDTIEQFGGKV-NDAAPVSOSA-N (2r,3r)-2,3-dihydroxybutanedioic acid;2-[(3s)-piperidin-3-yl]isoindole-1,3-dione Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O.O=C1C2=CC=CC=C2C(=O)N1[C@H]1CCCNC1 NLKBDTIEQFGGKV-NDAAPVSOSA-N 0.000 claims 1
- 125000006280 2-bromobenzyl group Chemical group [H]C1=C([H])C(Br)=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000006282 2-chlorobenzyl group Chemical group [H]C1=C([H])C(Cl)=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000004847 2-fluorobenzyl group Chemical group [H]C1=C([H])C(F)=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000006481 2-iodobenzyl group Chemical group [H]C1=C([H])C(I)=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000006179 2-methyl benzyl group Chemical group [H]C1=C([H])C(=C(C([H])=C1[H])C([H])([H])*)C([H])([H])[H] 0.000 claims 1
- POAZMSVKCTYEPJ-UHFFFAOYSA-N 2-piperidin-3-ylisoindole-1,3-dione Chemical compound O=C1C2=CC=CC=C2C(=O)N1C1CCCNC1 POAZMSVKCTYEPJ-UHFFFAOYSA-N 0.000 claims 1
- 102000055006 Calcitonin Human genes 0.000 claims 1
- 108060001064 Calcitonin Proteins 0.000 claims 1
- KZBUYRJDOAKODT-UHFFFAOYSA-N Chlorine Chemical compound ClCl KZBUYRJDOAKODT-UHFFFAOYSA-N 0.000 claims 1
- FEWJPZIEWOKRBE-LWMBPPNESA-L D-tartrate(2-) Chemical compound [O-]C(=O)[C@@H](O)[C@H](O)C([O-])=O FEWJPZIEWOKRBE-LWMBPPNESA-L 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- 206010018429 Glucose tolerance impaired Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 208000001280 Prediabetic State Diseases 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- BBBFJLBPOGFECG-VJVYQDLKSA-N calcitonin Chemical compound N([C@H](C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H]([C@@H](C)O)C(=O)N1[C@@H](CCC1)C(N)=O)C(C)C)C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 BBBFJLBPOGFECG-VJVYQDLKSA-N 0.000 claims 1
- 229960004015 calcitonin Drugs 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 239000007943 implant Substances 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000004923 naphthylmethyl group Chemical group C1(=CC=CC2=CC=CC=C12)C* 0.000 claims 1
- 125000006504 o-cyanobenzyl group Chemical group [H]C1=C([H])C(C#N)=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000006513 pyridinyl methyl group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 150000003459 sulfonic acid esters Chemical class 0.000 claims 1
- 238000003786 synthesis reaction Methods 0.000 claims 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
- C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
- A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07—ORGANIC CHEMISTRY
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- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Hydrogenated Pyridines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Claims (15)
1. Postupak proizvodnje lijeka, naznačen time, da obuhvaća uporabu spoja opće formule (I):
[image]
ili njegovog enantiomera ili njegove soli,
gdje R1 je jedna od skupina fenilkarbonilmetil, benzil, naftilmetil, piridinilmetil, pirimidinilmetil, kinolinilmetil, izokinolinilmetil, kinazolinilmetil, kinoksalinilmetil, naftiridinilmetil ili fenantridinilmetil, u kojoj aromatski ili heteroaromatski dio u svakom slučaju je mono-ili je disupstituiran s Ra, gdje supstituenti mogu biti isti ili različiti i
Ra je atom vodika, fluora, klora ili broma ili jedna od skupina cijano, metil, trifluorometil, etil, fenil, metoksi, difluorometoksi, trifluorometoksi ili etoksi,
ili dvije skupine Ra, kada su one vezane na susjedne atome ugljika, mogu također biti -O-CH2-O-skupina ili -O-CH2-CH2-O-skupina,
R2 je jedna od skupina metil, etil, propil, izopropil, ciklopropil ili fenil i
R3 je jedna od skupina 2-buten-1-il, 3-metil-2-buten-1-il, 2-butin-1-il, 2-fluorobenzil, 2-klorobenzil, 2-bromobenzil, 2-jodobenzil, 2-metilbenzil, 2-(trifluorometil)benzil ili 2-cijanobenzil,
dobivena pomoću postupka koji obuhvaća sljedeće korake sinteze:
a) reakcija spoja opće formule (III)
[image]
pri čemu je X izlazna skupina odabrana iz skupine halogena ili estera sulfonske kiseline i
R1 do R3 su određeni kao što je gore navedeno,
s 3-(ftalimido)piperidinom ili njegovim enantiomerom,
b) odstranjivanje zaštite spoja opće formule (II) koji je tako dobiven
[image]
pri čemu su R1 do R3 određeni kao što je gore navedeno, i
c) opcijski, pretvaranje u fiziološki prihvatljivu sol;
i opcijski jednog ili više inertnih nosača i/ili razrjeđivača.
2. Postupak proizvodnje lijeka prema zahtjevu 1, naznačen time, da
X je atom broma,
R1 je skupina (4-metil-kinazolin-2-il)metil, (3-metil-izokinolin-1-il)metil ili (3-cijanopiridin-2-il)metil,
R2 je metil-skupina i
R3 je 2-butin-1-il-skupina.
3. Postupak proizvodnje lijeka prema zahtjevu 1 ili 2, naznačen time, da se (R)-3(ftalimido)piperidin upotrebljava kao reakcijsko sredstvo u koraku a).
4. Postupak proizvodnje lijeka prema zahtjevu 3, naznačen time, da
X je atom broma,
R1 je (4-metil-kinazolin-2-il)metil-skupina,
R2 je metil-skupina i
R3 je 2-butin-1-il-skupina.
5. Postupak proizvodnje lijeka prema zahtjevu 4, naznačen time, da nadalje obuhvaća kristalizaciju spoja formule (I) iz otopine metanola ili etanola.
6. Postupak proizvodnje lijeka prema zahtjevu 5, naznačen time, da otopina nadalje sadrži tert-butilmetileter.
7. Postupak proizvodnje lijeka prema zahtjevu 4, naznačen time, da postupak za proizvodnju spoja formule (I) obuhvaća uglavnom kristalizaciju spoja formule (I) iz etanola.
8. Spoj, naznačen time, da je to (R)-3-(ftalimido)piperidin D-tartrat ili (S)-3-(ftalimido)piperidin L-tartrat.
9. Postupak proizvodnje lijeka, naznačen time, da obuhvaća uporabu spoja opće formule
[image]
ili njegovog enantiomera, gdje
R1 je (4-metil-kinazolin-2-il)metil-skupina,
R2 je metil-skupina i
R3 je 2-butin-1-il-skupina,
dobivena postupkom prema jednom od zahtjeva 4 do 7;
i opcijski jednog ili više inertnih nosača i/ili razrjeđivača.
10. Postupak proizvodnje lijeka, naznačen time, da obuhvaća uporabu spoja prema zahtjevu 9, dobivenog pomoću postupka prema zahtjevu 7, te opcijski jednog ili više inertnih nosača i/ili razrjeđivača.
11. Postupak proizvodnje lijeka prema jednom od zahtjeva 1 do 3, naznačen time, da je lijek pogodan za liječenje dijabetes melitusa tipa I i tipa II, pred-dijabetesa ili smanjene tolerancije na glukozu, artritisa, pretilosti, odbijanja transplantiranih usadaka i osteoporoze prouzročene kalcitoninom.
12. Postupak proizvodnje lijeka, naznačen time, da obuhvaća uporabu spoja opće formule (I) ili njegovog enantiomera, pri čemu su R1 do R3 određeni kao u jednom od zahtjeva 1 do 2, dobivenog u postupku koji obuhvaća odstranjivanje zaštite spoja opće formule (II) kao što je pokazano u zahtjevu 1, gdje su R1 do R3 određeni kao u jednom od zahtjeva 1 do 2, ili njegovog enantiomera;
i opcijski jednog ili više inertnih nosača i/ili razrjeđivača.
13. Postupak proizvodnje lijeka, naznačen time, da obuhvaća uporabu spoja sljedeće formule (I)
[image]
gdje
R1 je (4-metil-kinazolin-2-il)metil-skupina,
R2 je metil-skupina i
R3 je 2-butin-1-il-skupina,
dobiven pomoću postupka koji obuhvaća odstranjivanje zaštite spoja sljedeće formule (II)
[image]
gdje
R1 je (4-metil-kinazolin-2-il)metil-skupina,
R2 je metil-skupina i
R3 je 2-butin-1-il-skupina,
i opcijski jednog ili više inertnih nosača i/ili razrjeđivača.
14. Postupak proizvodnje lijeka prema zahtjevu 13, naznačen time, da nadalje obuhvaća kristalizaciju spoja formule (I) iz otopine etanola.
15. Postupak proizvodnje lijeka prema zahtjevu 13 ili 14, naznačen time, da se odstranjivanje zaštite od ftalil-zaštitne skupine spoja formule (II), provodi u prisutnosti etanolamina, poželjno u mješavini tetrahidrofurana i vode ili u toluenu.
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DE102004054054A DE102004054054A1 (de) | 2004-11-05 | 2004-11-05 | Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine |
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