PL408029A1 - Cyclic derivatives of zoledronic acid and method of their production - Google Patents
Cyclic derivatives of zoledronic acid and method of their productionInfo
- Publication number
- PL408029A1 PL408029A1 PL408029A PL40802914A PL408029A1 PL 408029 A1 PL408029 A1 PL 408029A1 PL 408029 A PL408029 A PL 408029A PL 40802914 A PL40802914 A PL 40802914A PL 408029 A1 PL408029 A1 PL 408029A1
- Authority
- PL
- Poland
- Prior art keywords
- zoledronic acid
- cyclic
- evaporated
- reacted
- integer
- Prior art date
Links
- 125000004122 cyclic group Chemical group 0.000 title abstract 2
- 229960004276 zoledronic acid Drugs 0.000 title abstract 2
- WSFSSNUMVMOOMR-UHFFFAOYSA-N Formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 abstract 6
- -1 cyclic zoledronic acid derivatives Chemical class 0.000 abstract 3
- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 abstract 2
- LEQAOMBKQFMDFZ-UHFFFAOYSA-N glyoxal Chemical compound O=CC=O LEQAOMBKQFMDFZ-UHFFFAOYSA-N 0.000 abstract 2
- BGJSXRVXTHVRSN-UHFFFAOYSA-N 1,3,5-trioxane Chemical compound C1OCOCO1 BGJSXRVXTHVRSN-UHFFFAOYSA-N 0.000 abstract 1
- 229910021529 ammonia Inorganic materials 0.000 abstract 1
- 239000007864 aqueous solution Substances 0.000 abstract 1
- 229940015043 glyoxal Drugs 0.000 abstract 1
- 229910017053 inorganic salt Inorganic materials 0.000 abstract 1
- 150000007522 mineralic acids Chemical class 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 229920002866 paraformaldehyde Polymers 0.000 abstract 1
- FAIAAWCVCHQXDN-UHFFFAOYSA-N phosphorus trichloride Chemical compound ClP(Cl)Cl FAIAAWCVCHQXDN-UHFFFAOYSA-N 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1
Abstract
Przedmiotem wynalazku są cykliczne pochodne kwasu zoledronowego przedstawione wzorem ogólnym 1, w którym n oznacza liczbę całkowitą od 1 do 4. Wynalazek ujawnia również sposób wytwarzania cyklicznych pochodnych kwasu zoledronowego przedstawionych wzorem ogólnym 1, w którym n oznacza liczbę całkowitą od 1 do 4 polegający na tym, że cykliczny aminokwas o wzorze 2, w którym n ma znaczenie jak podane poprzednio, poddaje się reakcji z co najmniej jedną częścią glioksalu, co najmniej jedną częścią amoniaku, co najmniej jedną częścią formaldehydu wybranego z grupy obejmującej formalinę, trioksan i paraform oraz co najmniej jedną częścią zasady, w temperaturze 273-373 K, po czym z mieszaniny odparowuje się lotne składniki pod zmniejszonym ciśnieniem w temperaturze 293-373 K, a tak otrzymaną pozostałość neutralizuje się wodnym roztworem kwasu nieorganicznego, oddziela się powstałą sól nieorganiczną i odparowuje do sucha pod zmniejszonym ciśnieniem w temperaturze 293-373 K; otrzymaną pozostałość rozpuszcza się w wodzie, poddaje się reakcji z trójchlorkiem fosforu, następnie hydrolizuje i wydziela się cykliczne pochodne kwasu zoledronowego.The invention relates to cyclic zoledronic acid derivatives represented by the general formula 1, wherein n is an integer from 1 to 4. The invention also discloses a method of producing cyclic zoledronic acid derivatives represented by the general formula 1, wherein n is an integer from 1 to 4 that the cyclic amino acid of formula 2 in which n is as previously described is reacted with at least one part of glyoxal, at least one part of ammonia, at least one part of formaldehyde selected from the group consisting of formalin, trioxane and paraform, and at least one part of the base at 273-373 K, after which the volatile components are evaporated from the mixture under reduced pressure at 293-373 K, and the residue thus obtained is neutralized with an aqueous solution of inorganic acid, the resulting inorganic salt is separated and evaporated to dryness under reduced pressure em at a temperature of 293-373 K; the residue obtained is dissolved in water, reacted with phosphorus trichloride, then hydrolysed and the cyclic derivatives of zoledronic acid are isolated.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PL408029A PL408029A1 (en) | 2014-04-28 | 2014-04-28 | Cyclic derivatives of zoledronic acid and method of their production |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PL408029A PL408029A1 (en) | 2014-04-28 | 2014-04-28 | Cyclic derivatives of zoledronic acid and method of their production |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PL408029A1 true PL408029A1 (en) | 2015-02-16 |
Family
ID=52464737
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PL408029A PL408029A1 (en) | 2014-04-28 | 2014-04-28 | Cyclic derivatives of zoledronic acid and method of their production |
Country Status (1)
| Country | Link |
|---|---|
| PL (1) | PL408029A1 (en) |
-
2014
- 2014-04-28 PL PL408029A patent/PL408029A1/en unknown
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