184704. lajstromszámú szabadalom • Eljárás biológiailag aktív enkefalin analógok előállítására

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H.Arg.Tyr.Gly.Gly.Phe.Leu.OH 2HC1 H.Tyr.Ala.D.Ala.Phe.Met.Ome HG H.Tyr.GIa.D-AlaJPhe.Met.OMe HG H.Tyr.Ala.D-Ala.Phe.Met.OH HG H.Tyr.Gly.D-Ala.Phe.Met.OH HG H,Arg.Tyr.Gly.Gly.Phe.Leu.Thr.OH 2HG H.Tyr.D-Ala.Gly.Phe.Pro.OH HG H.Tyr.D-Ala.D-Ala.Phe.Leu.OH HG H.Tyr.D-Ala.Gly.Leu.Leu.OH HG H.Tyr.De.Asn.Met.Leu.OH H.Tyr.Ala.Gly.Phe.Leu.OH HG H.Tyr.Gly.Gly.Phe.Nle.OH HG H.Tyr.D-Leu.Gly.Phe.Leu.OH HG H.Tyr.Ala.Ala.Phe.Leu.OH HG H.Tyr.Gly.Pro.Phe.Leu.OH HG H.Tyr.D-Ala.Gly.D.Phe.Leu.OH HG H.Tyr.Gly.Gly.Phe.D-Leu.OH HG H.Tyr.Gly.Gly.D-Phe.Leu.OH HG H.Tyr.Gly.Gly.Phe.De.OH HG H.Tyr.D-Ala.Gly.C-fenilglicil-Leu.OH HG H .Phe ,D-Alá .Gly .Phe. Le u.OH HG H.Tyr.D-Ala.Sar.Phe.Leu.OMe HG H.Tyr.Gly.Ala.Phe.Leu.OH HG H.Tyr.D-Ala.Gly.Phe.Thr.OH HG H.Tyr.D-Ala.Asn.Phe.Leu.OH HG H.Tyr.D.Ala.Gly.Phe.D-Leu.OMe HG H.Tyr.D-Ala.Gly.Phe.D-Leu.OH HG Ac

H.Tyr.D-Ala.Gly.Phe.Leu.OH HG Ac

0.382,0,614,

o.582,o.973,o.884

o.6i2,o,983,o.854

0,582,0,543,0,614

0.502,0,553,0,564

0.152,0,323,0:514

0.442

0.682,0.933,0.934 0.682,0.743,0.884 0.572, Ö.834 0.552, Ö.843,0.864 0.582,0.853,0.864 0.851,0.862,0.793 0.761,0.622,0.743 O^.O^.OJS3 0,572,0.863 O^.O^.O^3 0,512,0,853,0,484 o.76‘,o.852,o.653 0.642,0.853 0.662,0,933 0.642,0.904 0.622,0.863,0.634 0.502,0.514 O^.O^.O^4 0.632,0.924 0.572,0.933,0.824

0.602,0.943,0.854

+17>7 O(c=0,52)' -3,66° (c=0,2) +30,19° (c=0,2) +4,22°

+34,19'

+1,63 -1,52°

+43.71'

—4,43°-13,5°-1,35°

+24,44'

+17,3°-33,6°-30,0°

+27,2°

+28,7°

+24,5°

+22,7°

+43,7°

+21,2°

+3,69°-12,07

00,5)

(c=0,51)

(c=l)

00,5)

(c=0,2)

(c=l)

(c=0,4)

(c=0.2)

(c=0,6)

00,5)

+19,8

+6,26°

+39,6°

+31,5°

00,52)

(c=0,6)

(c=0,48

00,52

,00,4)

’ OD

0=0,51)

(c=0,49)

00,51)

(c=0,53)

+14,6° (c=0,5)

-Tyr-=04 -acetiltirozil H.Tyr.D-Ala.Sar.Phe.Leu.OH HC1 H.Tyr.D-Ala-Gly.Phe.Leu.Thr.OH HG H.MeTyr.Gly.Gly.Phe.Leu.OH HG H.Tyr.D-Ala.Gly.Phe.Nle.OH HG H.Tyr.Gly.Sar.Phe.Leu.OMe HG H.Tyr.Gly.Sar.Phe.Leu.OMe HG H.D-Tyr.D-Ala.Gly.Phe.Leu.OH HG H.D-Tyr.D-Ala.Gly.Phe.D-Leu.OH HG H.Tyr.Gly.Sar.Phe.Leu.OH HC1 H.Tyr.D-Ala.Gly.Phe.D-Leu.Thr.OH HG H.Tyr.D-Ala.Gly.Phe.D.Met.OH HG H.Tyr.Pro.Gly.Phe.Leu.OH HG . H.Tyr.D-Ala.Gly.Phe.D-Met.Thi.OH HG H.Tyr.Sar.Gly.Phe.Leu.OH HG H.Me.Tyr.D-Ala.Gly.Phe.Leu.OH H.Tyr.gly.D-Pro.Phe.Leu.OH HG

0.582,0.854 0.552,0.933, 0.724 0.572,0.643,0.644 0.522,0.684. 0.562,0.703,0.904 0.562,0.703,0.904 0.552,0.683 0.572,0.623,0.504 0.592,0.803,0.684 0.512,0.663,0.554 0.552,0.673, 0.584,0.825 0.923,0.764,0.66s 0.612,0,763.

0.723,0.914,0.542 0.904,0,853,0.522 0.894, 0.823j 0.592

H.Tyr.D-Ala.D-Pro.Phe.Leu.OH nátrium só 0,744,0.Sl^.O^2!

H.Metyr.Gly.Gly.Phe.Leu.OMe HG H.MeTyr.D-Ala.Gly.Phe.Leu.OMe HG H.Tyr.D-MeAla.Gly.Phe.D-Leu.OMe HG H.Tyr.D-MeAla.gly.Phe.D-Leu.OH HG H.Tyr.D-Ala.Gly.Phe.Leu.OMe HG H.Tyr.D-Ala.Gly.Phe.D-Met.OMe HG M.D-Tyr.Gly.Gly.Phe.Leu.OH HG H.MeTyr.D-Ala.Gly.Phe.D-Leu.OH HG 0.55: H.MeTyr.D-Ala.Gly.Phe.D-Leu.OMe HG 0.52" H.DOPA.Gly.Gly.Phe.Leu.OH HG 0.49;

DOPA =3,4-diíiidroxifenilalanil H.Tyr.MeAla.Gly.Phe.D-Leu.OH HG 0.515

H.Tyr.D-Ala.Gly.Phe.D-Leu.D-Thr.OH HG0.502

0.984,0.993,0.482

o^.o^.o^2

0.914,0.853,0.602 0.684,0,723,0.622 0.954,0.953,0.632 0.944, Q.933,0.572 0.582

+9,89°

+5,13°

+25,5°

+23,2°

\10-S

+10,2° (c=0.4) 3,5)

(c=1) (c=0,5) (c=0,5) (c-1,0)-20,7° (c=0,í ,51° (c=0,5) (c=l,0) (c=0,52) (c=0,51) (c=0,2) (c=0,51) (c=0,l)

+17,1

+51,5°

+31,0°-5’6°o

+47,5°

+20,5°

+61,3C +49,9C ♦11,6*

(c=0.39)

(c=0,45)

(c=0,44)

+37,8° (c=0,38)

H.D-Tyr.Gly.Gly.Phe.Leu.OMe HG H.Tyr.MeAla.Gly.Phe.D-Leu.OMe HG H.Tyr.D-Ala.Gly.Phe.D-Leu.NHEt HG H.MeTyr.D-Ala.Giv.Phe.D-Leu.NHEt HG

0.632 0,592-39,0° 01,0)

, 0.813,

, 0.824

+40,9°

OD

, 0.903,

, 0.92*

+54,7°

Oi)

, 0.853

+13,8° 00,4)

,0.883,

, 0.794

+17° 1

01,0)

+48,9° 1

fc=0,5)

, 0.973,

, 0.934-42,7° J

fc=0,1 )

+9.03° 1

c=0.2)

, 0.934,

0.61s

+46,5° 1

íc=0,5)

. 0.923.

0.964

+50.0°

OU

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