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. 2023 Feb 15;11(2):564. doi: 10.3390/biomedicines11020564

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© 2023 by the authors.

Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).

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Scheme 1 — Synthesis strategy of conjugate 1 (path I) and 2 (path II) by SPPS method. (a)—30% piperidine in DMF, (b)—Fmoc-Pro-OH:DIC:HOBt, (c)—Fmoc-Leu-OH:DIC:HOBt, (d)—Fmoc-Trp(Boc)-OH:DIC:HOBt, (e)—Fmoc-Thr(tBu)-OH:DIC:HOBt, (f)—Fmoc-Ala-OH:DIC:HOBt, (g)—Fmoc-Ahx-OH:DIC:HOBt, (h)—DOTA-tris(tBu)-NHS:triethylamine, (i)—TFA/PhOH/H₂O/TIPS, (j)—Fmoc-L-Dab(Alloc)-OH:DIC:HOBt, (k)—Boc-Lys(Fmoc)-OH:DIC:HOBt, (l)—di-Boc-S-methylisothiourea:n-butylamine:DCM, (m)—phenylsilane:tetrakis(triphenylphosphine)-palladium:DCM [41].