HRP20211031T1 - Postupak za proizvodnju novog spoja koji sadrži dušik ili njegove soli i proizvodnja njihovog međuprodukta - Google Patents

Postupak za proizvodnju novog spoja koji sadrži dušik ili njegove soli i proizvodnja njihovog međuprodukta Download PDF

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HRP20211031T1
HRP20211031T1 HRP20211031TT HRP20211031T HRP20211031T1 HR P20211031 T1 HRP20211031 T1 HR P20211031T1 HR P20211031T T HRP20211031T T HR P20211031TT HR P20211031 T HRP20211031 T HR P20211031T HR P20211031 T1 HRP20211031 T1 HR P20211031T1
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Hirofumi Fukunaga
Sachiko SHINJO
Daisuke Nakagawa
Shinichiro SEKINE
Takayuki Yamakawa
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Fujifilm Corporation
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Claims (19)

1. Postupak proizvodnje spoja predstavljenog s formulom [11] ili njegove soli, koji obuhvaća: (1) korak reakcije spoja prikazanog formulom [1] ili njegove soli [image] u formuli, R1 predstavlja vodikov atom ili amino zaštitnu skupinu; R2 predstavlja karboksilnu zaštitnu skupinu; L1 predstavlja skupinu prikazanu s formulom [2a] [image] u formuli, R3a, R4a, R5a i R6a su jednaki ili se međusobno razlikuju i predstavljaju vodikov atom ili skupinu C1-6 alkil; p1 predstavlja cijeli broj od 1 do 3; q1 predstavlja cijeli broj od 0 do 3; i r1 predstavlja cijeli broj od 1 do 6; i L2 predstavlja skupinu prikazanu s formulom [2b] [image] u formuli, R3b, R4b, R5b i R6b su jednaki ili se međusobno razlikuju i predstavljaju vodikov atom ili skupinu C1-6 alkil; p2 predstavlja cijeli broj od 1 do 3, q2 predstavlja cijeli broj od 0 do 3; i r2 predstavlja cijeli broj od 1 do 6; sa spojem predstavljenim formulom [3] ili njegovom soli [image] u formuli, L3 predstavlja skupinu prikazanu s formulom [2c] [image] u formuli, R3c, R4c, R5c i R6c su jednaki ili se međusobno razlikuju i predstavljaju vodikov atom ili skupinu C1-6 alkil; p3 predstavlja cijeli broj od 1 do 3; q3 predstavlja cijeli broj od 0 do 3; i r3 predstavlja cijeli broj od 1 do 6; A1 predstavlja bilo koju od skupina koju predstavljaju formule [4] do [9] [image] u formulama, * predstavlja vezujući položaj; i R7 su jednaki ili se međusobno razlikuju i predstavljaju karboksilnu zaštitnu skupinu; i m predstavlja cijeli broj od 1 do 3; tako da se dobije spoj predstavljen formulom [10] ili njegova sol; [image] u formuli, R1, R2, L1, L2, L3, A1, i m imaju istu definiciju kao R1, R2, L1, L2, L3, A1, i m opisani gore; i (2) korak uklanjanja zaštite spoja predstavljenog formulom [10] ili njegove soli, [image] (3) u formuli, A2 predstavlja bilo koju od skupina koju predstavljaju Formule [12] do [17] [image] u formulama, * predstavlja vezujući položaj; i L1, L2, L3, i m imaju istu definiciju kao L1, L2, L3, i m opisani gore.
2. Postupak proizvodnje prema patentnom zahtjevu 1, naznačen time što R2 je skupina C1-6 alkil koja može biti supstituirana ili benzilna skupina koja može biti supstituirana.
3. Postupak proizvodnje prema patentnom zahtjevu 1 ili 2, naznačen time što L3 je skupina predstavljena s formulom [18c] [image] u formuli, R5c i R6c mogu biti jednaki ili se razlikuju jedan od drugog i predstavljaju vodikov atom ili skupinu C1-6 alkil; i r3 predstavlja cijeli broj od 1 do 6.
4. Postupak proizvodnje prema bilo kojem od patentnih zahtjeva 1 do 3, naznačen time što L1 je skupina predstavljena s formulom [18a] [image] u formuli, R5a i R6a su jednaki ili se međusobno razlikuju i predstavljaju vodikov atom ili skupinu C1-6 alkil; i r1 predstavlja cijeli broj od 1 do 6.
5. Postupak proizvodnje prema bilo kojem od patentnih zahtjeva 1 do 4, naznačen time što L2 je skupina predstavljena s formulom [18b] [image] u formuli, R5b i R6b su jednaki ili se međusobno razlikuju i predstavljaju vodikov atom ili skupinu C1-6 alkil; i r2 predstavlja cijeli broj od 1 do 6.
6. Postupak proizvodnje prema bilo kojem od patentnih zahtjeva 1 do 5, naznačen time što R1 je vodikov atom, skupina C1-6 alkoksikarbonil koja može biti supstituirana, arilsulfonilna skupina koja može biti supstituirana, ili heterociklička sulfonilna skupina koja može biti supstituirana.
7. Postupak proizvodnje prema bilo kojem od patentnih zahtjeva 1 do 6, naznačen time što R7 je skupina C1-6 alkil koja može biti supstituirana ili benzilna skupina koja može biti supstituirana.
8. Postupak proizvodnje prema bilo kojem od patentnih zahtjeva 1 do 7, naznačen time što je korak uklanjanja zaštite korak uklanjanja zaštite upotrebom kiseline.
9. Postupak za proizvodnju od metalnog kompleksa, naznačen time što obuhvaća: korak reakcije spoja prikazanog formulom [11] ili njegove soli koja je dobivena postupkom proizvodnje prema bilo kojem od patentnih zahtjeva 1 do 7 s metalnim ionom.
10. Postupak proizvodnje prema patentnom zahtjevu 9, naznačen time što je spoj predstavljen s formulom [11] ili njegova sol 2,2',2"-(10-(2-(((R)-1-((2-(4-(4-(N-((S)-1-karboksi-2-(5-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)pentanamido)etil)sulfamoil)-3,5-dimetilfenoksi)butanamido)etil)amino)-l-okso-3-sulfopropan-2-il)amino)-2-oksoetil)-1,4,7,10-tetraazaciklododekan-1,4,7-triil)trioctena kiselina ili njezina sol i metalni ion je radioaktivni metalni ion.
11. Spoj predstavljen s formulom [19] ili njegova sol [image] u formuli, R1 predstavlja vodikov atom ili amino- zaštitnu skupinu odabranu iz skupine koju čine skupina Ar C1-6 alkil, skupina C1-6 alkoksi C1-6 alkil, acilna skupina, skupina C1-6 alkoksikarbonil, skupina Ar C1-6 alkoksikarbonil, ariloksikarbonilna skupina, skupina C1-6 alkilsulfonil, heterociklička sulfonilna skupina, arilsulfonilna skupina, i silil skupina, koja može biti supstituirana s jednim ili više supstituenata odabranih iz skupine supstituenata A, pri čemu skupina supstituenata A sadrži halogeni atom, nitro skupinu, cijano skupinu, amino skupinu, hidroksilnu skupinu, skupinu C1-6 alkil, skupinu C3-8 cikloalkil, arilnu skupinu, C1-6 alkoksi skupinu, C1-6 alkilamino skupinu, di(C1-6 alkil)amino skupinu, heterocikličku skupinu, i oksi skupinu; R8 predstavlja skupinu C2-6 alkil koja može biti supstituirana ili benzilnu skupinu koja može biti supstituirana; R9 predstavlja skupinu prikazanu s formulom [20] [image] u formuli, * predstavlja vezujući položaj; R10 predstavlja hidroksilnu skupinu ili skupinu prikazanu s formulom [21] [image] u formuli, * predstavlja vezujući položaj, L3 predstavlja skupinu prikazanu s formulom [2c] [image] u formuli, R3c, R4c, R5c, i R6c su jednaki ili se međusobno razlikuju i predstavljaju vodikov atom ili skupinu C1-6 alkil; p3 predstavlja cijeli broj od 1 do 3; q3 predstavlja cijeli broj od 0 do 3; i r3 predstavlja cijeli broj od 1 do 6; A1 predstavlja bilo koju od skupina koju predstavljaju Formule [4] do [9] [image] u formulama, * predstavlja vezujući položaj; i R7 predstavlja karboksilnu zaštitnu skupinu; i m predstavlja cijeli broj od 1 do 3; L2 predstavlja skupinu prikazanu s formulom [2b] [image] u formuli, R3b, R4b, R5b i R6b su jednaki ili se međusobno razlikuju i predstavljaju vodikov atom ili skupinu C1-6 alkil; p2 predstavlja cijeli broj od 1 do 3; q2 predstavlja cijeli broj od 0 do 3; i r2 predstavlja cijeli broj od 1 do 6; i L1 predstavlja skupinu prikazanu s formulom [2a] [image] u formuli, R3a, R4a, R5a i R6a su jednaki ili se međusobno razlikuju i predstavljaju vodikov atom ili skupinu C1-6 alkil; p1 predstavlja cijeli broj od 1 do 3; q1 predstavlja cijeli broj od 0 do 3; i r1 predstavlja cijeli broj od 1 do 6.
12. Spoj prema patentnom zahtjevu 11 ili njegova sol, naznačen time što R8 je skupina C2-6 alkil koja može biti supstituirana.
13. Spoj prema patentnom zahtjevu 11 ili 12 ili njegova sol, naznačen time što L3 je skupina predstavljena s formulom [18c] [image] u formuli, R5c i R6c su jednaki ili se međusobno razlikuju i predstavljaju vodikov atom ili skupinu C1-6 alkil; i r3 predstavlja cijeli broj od 1 do 6.
14. Spoj prema bilo kojem od patentnih zahtjeva 11 do 13 ili njegova sol, naznačen time što L1 je skupina predstavljena s formulom [18a] [image] u formuli, R5a i R6a su jednaki ili se međusobno razlikuju i predstavljaju vodikov atom ili skupinu C1-6 alkil; i r1 predstavlja cijeli broj od 1 do 6.
15. Spoj prema bilo kojem od patentnih zahtjeva 11 do 14 ili njegova sol, naznačen time što L2 predstavlja skupinu prikazanu s formulom [18b] [image] u formuli, R5b i R6b su jednaki ili se međusobno razlikuju i predstavljaju vodikov atom ili skupinu C1-6 alkil; i r2 predstavlja cijeli broj od 1 do 6.
16. Spoj prema bilo kojem od patentnih zahtjeva 11 do 15 ili njegova sol, naznačen time što R1 je vodikov atom, skupina C1-6 alkoksikarbonil koja može biti supstituirana, arilsulfonilna skupina koja može biti supstituirana, ili heterociklička sulfonilna skupina koja može biti supstituirana.
17. Spoj prema bilo kojem od patentnih zahtjeva 11 do 16 ili njegova sol, naznačen time što R7 je skupina C1-6 alkil koja može biti supstituirana ili benzilna skupina koja može biti supstituirana.
18. Spoj predstavljen s formulom [3] ili njegova sol [image] u formuli, L3 predstavlja skupinu prikazanu s formulom [2c] [image] u formuli, R3c, R4c, R5c i R6c su jednaki ili se međusobno razlikuju i predstavljaju vodikov atom ili skupinu C1-6 alkil; p3 predstavlja cijeli broj od 1 do 3; q3 predstavlja cijeli broj od 0 do 3; i r3 predstavlja cijeli broj od 1 do 6; A1 predstavlja bilo koju od skupina koju predstavljaju Formule [4] do [9] [image] u formulama, * predstavlja vezujući položaj; i R7 predstavlja karboksilnu zaštitnu skupinu; i m predstavlja cijeli broj od 1 do 3.
19. Spoj prema patentnom zahtjevu 18 ili njegova sol, naznačen time što R7 je skupina C1-6 alkil koja može biti supstituirana ili benzilna skupina koja može biti supstituirana.
HRP20211031TT 2015-03-25 2021-06-29 Postupak za proizvodnju novog spoja koji sadrži dušik ili njegove soli i proizvodnja njihovog međuprodukta HRP20211031T1 (hr)

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