- Synthetic process of homodimer of FKBP ligand
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The invention discloses a synthesis process of homodimer of FKBP ligand and belongs to an improved synthesis process of AP1903, wherein the homodimer of FKBP ligand refers to AP1903. According to theoptimized route of the synthesis process chooses, (S)-piperidine-2-methyl formate is connected to the compound Cpd9' as selected, an acid Cpd6' obtained after ester hydrolysis is easier to be purified by post-treatment purification, and precipitation or extraction treatment can be chosen by the post-treatment purification. Although the total reaction steps of the synthetic route in the prior literature are the same as the optimized route of the invention, the synthetic route in the prior literature belongs to the vertical route, and the post-treatment of the fifth, sixth and eighth steps requires column chromatography, thereby leading to a higher research and development cost. The optimized AP1903 synthetic route belongs to the parallel route, and the post-treatment is simpler and more advantageous for separation and purification, so that the cost of research and development is relatively low and the economic benefit is obviously superior to that of the synthetic route in the prior art.
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Paragraph 0030; 0044-0046
(2019/05/28)
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- An Inexpensive and Scalable Synthesis of Shld
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A synthesis of the important FKBP ligand Shld is reported. The synthesis avoids stoichiometric use of expensive and chiral reagents, maintains enantioselectivity and provides a high overall yield (39%). The main features in the method are enantioselective alkylation for preparation of the phenyl acetic acid moiety (building block A), catalytic enantioselective reduction for obtaining the chiral diaryl-1-propanol (building block C), and direct acylation of S-pipecolic tartrate rather than use of expensive Fmoc-pipecolic acid. The assembly of the building blocks A-C is reversed in comparison to previous synthesis, which also eliminates the need for protective groups.
- J?rgensen, Frederik Pr?stholm,Bols, Mikael
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p. 6050 - 6055
(2018/05/24)
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- METHODS AND COMPOSITIONS FOR THE SYNTHESIS OF MULTIMERIZING AGENTS
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The invention features methods and compositions for the synthesis of multimerizing agents.
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- Materials and methods involving conditional retention domains
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Materials and methods involving conditional retention domains (CRDs) are disclosed. Also disclosed are fusion proteins containing CRDs and cells expressing such fusion proteins. In addition, the invention provides novel methods for producing target proteins in vivo using fusion proteins containing conditional retention domains and methods for identifying novel CRDs.
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- Synthetic multimerizing agents
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New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formulaM-L-Qwhere M is a synthetic ligand for an FKBP protein
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