All-solid-phase method for synthesizing octreotide
A solid-phase synthesis, octreotide technology, applied in the field of pharmaceutical synthesis, can solve the problems of shortening the preparation time, reducing the production cost, etc., and achieve the effects of shortening the preparation time, reducing the production cost, high purity and total yield
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Embodiment 1
[0041] Embodiment 1: the synthesis of linear heptapeptide resin
[0042] Take 0.15 mol Fmoc-Cys (Trt) and 0.15 mol HOBt, and dissolve them with an appropriate amount of DMF; take another 0.15 mol DIC, slowly add it to the protected amino acid DMF solution under stirring, and stir and react at room temperature for 30 minutes to obtain the activated Protected amino acid solution, spare.
[0043] Take 0.05mol of Boc-Thr(Bzl)-OL-Merrifield resin (substitution value about 0.5mmol / g), deprotect with 30% TFA / DCM solution for 30 minutes, neutralize with DIEA / DCM solution, wash with DMF and DCM Filter, add the activated Fmoc-Cys (Trt) solution, stir at room temperature for 3 hours, remove the reaction solution, wash 3 times with DMF, wash 3 times with DCM, each washing time is 3min, and then use 20% PIP / DMF The solution was deprotected for 25 minutes, washed and filtered to complete the access of Fmoc-Cys(Trt).
[0044] Fmoc-Thr(tBu), Fmoc-Lys(Boc), Fmoc-D-Trp, Fmoc-Phe and Fmoc-Cys(...
Embodiment 2
[0045] Embodiment 2: the synthesis of linear heptapeptide resin
[0046] Take 0.15 mol Fmoc-Cys (Trt) and 0.15 mol HOBt, and dissolve them with an appropriate amount of DMF; take another 0.15 mol DIC, slowly add it to the protected amino acid DMF solution under stirring, and stir and react at room temperature for 30 minutes to obtain the activated Protected amino acid solution, spare.
[0047] Take 0.05mol of Boc-Thr(Bzl)-OL-Merrifield resin (substitution value about 0.5mmol / g), deprotect with 30% TFA / DCM solution for 30 minutes, neutralize with DIEA / DCM solution, wash with DMF and DCM Filter, add the activated Fmoc-Cys (Trt) solution, stir at room temperature for 3 hours, remove the reaction solution, wash 3 times with DMF, wash 3 times with DCM, each washing time is 3min, and then use 20% PIP / DMF The solution was deprotected for 25 minutes, washed and filtered to complete the access of Fmoc-Cys(Trt).
[0048] Insert Fmoc-Thr(tBu), Fmoc-Lys(Boc), Fmoc-D-Trp(Boc), Fmoc-Phe a...
Embodiment 3
[0049] Embodiment 3: the synthesis of linear heptapeptide resin
[0050] Take 0.15mol Fmoc-Cys (Acm) and 0.15mol HOBt, and dissolve it with an appropriate amount of DMF; take another 0.15mol DIC, slowly add it to the protected amino acid DMF solution under stirring, and stir and react at room temperature for 30 minutes to obtain the activated protected amino acid solution, set aside.
[0051] Take 0.05mol of Boc-Thr(Bzl)-OL-Merrifield resin (substitution value about 0.5mmol / g), deprotect with 30% TFA / DCM solution for 30 minutes, neutralize with DIEA / DCM solution, wash with DMF and DCM Filter, add the activated Fmoc-Cys (Trt) solution, stir at room temperature for 3 hours, remove the reaction solution, wash 3 times with DMF, wash 3 times with DCM, each washing time is 3min, and then use 20% PIP / DMF The solution was deprotected for 25 minutes, washed and filtered to complete the access of Fmoc-Cys (Acm).
[0052] Fmoc-Thr(tBu), Fmoc-Lys(Boc), Fmoc-D-Trp, Fmoc-Phe and Fmoc-Cys(...
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