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MF： C58H66N10O9
The present invention relates to a novel...
A rational drug design approach, capital...
![cyclo[Pro(4-OCO-NH-CH<sub>2</sub>-CH<sub>2</sub>-NH-Boc)-Phg-D-Trp(BoC)-Lys(Boc)-Tyr(Bzl)-Phe]](/upload/2025/11/7b1c5fdd-f9cf-4b18-8c68-d830b01fce32.png)
cyclo[Pro(4-OCO-NH-CH2-CH2-NH-Boc)-Phg-D-Trp(BoC)-Lys(Boc)-Tyr(Bzl)-Phe]
pasireotide
| Conditions | Yield |
|---|---|
|
With
chlorotriisopropylsilane; trifluoroacetic acid;
In
water;
at 5 - 10 ℃;
for 1h;
|
|
|
cyclo[Pro(4-OCO-NH-CH2-CH2-NH-Boc)-Phg-D-Trp(BoC)-Lys(Boc)-Tyr(Bzl)-Phe];
With
trifluoroacetic acid;
at 0 ℃;
for 0.5h;
With
acetic acid;
at 5 ℃;
for 15h;
|
3.1 g |
bis(trichloromethyl) carbonate
N-BOC-1,2-diaminoethane
cyclo(Phe-Pro(4-OH)-Phg-D-Trp(Boc)-Lys(Boc)-Tyr(Bzl))
pasireotide
| Conditions | Yield |
|---|---|
|
bis(trichloromethyl) carbonate; cyclo(Phe-Pro(4-OH)-Phg-D-Trp(Boc)-Lys(Boc)-Tyr(Bzl));
In
tetrahydrofuran;
for 1h;
N-BOC-1,2-diaminoethane;
With
dmap;
In
tetrahydrofuran;
at 20 ℃;
With
chlorotriisopropylsilane; trifluoroacetic acid;
In
water;
for 2h;
|
cyclo[Pro(4-OCO-NH-CH2-CH2-NH-Boc)-Phg-D-Trp(BoC)-Lys(Boc)-Tyr(Bzl)-Phe]
bis(trichloromethyl) carbonate
N-BOC-1,2-diaminoethane
