- Preparation of L-threoninol and its bisoxazoline derivative
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(R,R)-Threoninol was prepared in one step from L-threonine in 86% isolated yield. The product was regioselectively transformed into 2,2-bis[(4R,5R)4-(hydroxymethyl)-5-methyl-1,3-oxazolin-2-yl]propane in 42% isolated yield.
- Lutsenko, Serghey,Jacobsson, Ulla,Moberg, Christina
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- Generally Applicable, Convenient Solid-Phase Synthesis and Receptor Affinities of Octreotide Analogs
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Octreotide, an analogue of the hormone somatostatin, has applications as a therapeutic and imaging agent for somatostatin-positive tumors.We have developed a generally applicable, convenient stepwise solid-phase synthetic protocol for octreotide (D-Phe-Cy
- Edwards, W. Barry,Fields, Cynthia G.,Anderson, Carolyn J.,Pajeau, Tammy S.,Welch, Michael J.,Fields, Gregg B.
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Read Online
- Heterogeneous Catalytic Hydrogenation of Chiral Amino Acid Methyl Esters to Amino Alcohols with Retention of Configuration Over Mg-Modified Cu/ZnO/Al2O3 Catalyst
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Selective hydrogenation of amino acid methyl esters to chiral amino alcohols is an important and fascinating process. The CuZn0.3Mg0.1AlOx catalyst for the synthesis of chiral amino alcohols was prepared by the fractional
- Zhan, Bing,Zhang, Shuangshuang,Yu, Jun,Xiao, Xiuzheng,Guo, Xiaoming,Mao, Dongsen,Lu, Guanzhong
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p. 2160 - 2166
(2017/07/25)
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- Methods and compositions for monitoring polymer array synthesis
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VLSIPS? manufacturing processes are of increasing commercial importance. The present invention provides methods and compositions for monitoring the efficiency and quality of polymer synthesis in VLSIPS? arrays. Methods for monitoring polymer synthesis in an array on a substrate are provided. Monoisomeric labels for the labeling of synthetic polymer arrays are provided. Methods and compositions for post-synthetically labeling polymers in polymer arrays are also provided.
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- Stereoselective synthesis and anti-inflammatory activities of 6- and 7-membered dioxacycloalkanes
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A class of 5-trifluoroacetylamino-1,3-dioxacycloalkanes, 5-benzoylamino-1,3-dioxacycloalkanes, and 5-amino-1,3-dioxacycloalkane compounds were stereoselectively synthesized as potential anti-inflammatory drug candidates. The anti-inflammatory activities of these compounds were tested using the xylene-induced mouse ear edema model, from which multiple compounds possessing anti-inflammatory properties which surpass aspirin were identified; these compounds were then compared to establish structure-activity relationships.
- Gu, Keli,Bi, Lanrong,Zhao, Ming,Wang, Chao,Dolan, Cheryl,Kao, Michael C.,Tok, Jeffrey B.-H.,Peng, Shiqi
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p. 1339 - 1347
(2007/10/03)
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- Enantioselective incorporation of azobenzenes into oligodeoxyribonucleotide for effective photoregulation of duplex formation
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A drop in melting point of 21.5°C is induced by the UV-photolytic trans→cis isomerization of the duplex formed between an oligonucleotide bearing two D-threoninol-tethered azobenzene moieties (see picture) in the side chain and its complementary counterpa
- Asanuma, Hiroyuki,Takarada, Tohru,Yoshida, Takayuki,Tamaru, Daisuke,Liang, Xingguo,Komiyama, Makoto
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p. 2671 - 2673
(2007/10/03)
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- Synthesis of acyclic nucleoside and nucleotide analogues from amino acids: A convenient approach to a PMEA-PMPA hybrid
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Nonracemic amino alcohols derived from common amino acids have been used to assemble acyclic nucleoside and nucleotide analogues with control of absolute stereochemistry. Both (R)- and (S)-2-amino-1-propanol, readily available from D- or L-alanine, were used to prepare the nucleoside analogues (R)- and (S)-9-[1- methyl-2-hydroxyethyl]adenine, and then the nucleotide analogues (R)- and (S)-9-[1-methyl-2-phosphonomethoxyethyl]adenine. In a similar fashion, the CBz derivative of L-threonine was used to prepare first (1R,2R)-9-[1-hydroxymethyl-2-hydroxypropyl]adenine, and then the bis phosphonomethoxy derivative. The bis phosphonate derived from threonine represents a unique structural hybrid of PMEA and PMPA, both of which have well established antiviral activity. (C) 2000 Elsevier Science Ltd.
- Jeffery, Arlen L.,Kim, Jae-Hun,Wiemer, David F.
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p. 5077 - 5083
(2007/10/03)
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