101492-91-5Relevant articles and documents
Radiosynthesis of novel N-18F-labeled 18F-FHex-α-l-Glu and 18F-FHex-β-Glu
Wen, Fuhua,Liu, Shaoyu,Ma, Hui,Tang, Ganghua
, p. 222 - 230 (2020)
N-18F-labeled amino acids are important substitutes for new positron emission tomography (PET) imaging tracers complementing the deficiency of 18F-fluorodeoxyglucose (18F-FDG). In this work, two novel N-6-18F-alkyl amino acid imaging agents, 18F-FHex-α-l-Glu and 18F-FHex-β-Glu, were designed and synthesized as potential probes for PET imaging of tumors. 18F-FHex-α-l-Glu was synthesized using the precursor 6 from 18F-F? with the yield of 16 ± 4% (n = 5, uncorrected) within about 50 minutes. The specific activity was 14.5 GBq/μmol, and the radiochemical purity was more than 95%. 18F-FHex-β-Glu was synthesized using the precursor 12 based on 18F-F? with the yield of 11 ± 3% (n = 3, uncorrected) in about 60 minutes. The specific activity was 9.1 GBq/μmol, and the radiochemical purity was more than 95%.
Concise synthesis of hydroxy β -methyl fatty acid ethyl esters
Sakai, Yuki,Asakura, Yukiko,Morita, Mitsuhiro,Takahashi, Takashi
, p. 1195 - 1198 (2017)
Hydroxy β-methyl fatty acid ethyl esters bearing different carbon chain lengths and varying hydroxyl group positions were successfully synthesized from symmetric diols. These fatty acid derivatives are useful intermediates of chemical probes for metabolic
Synthesis of fused bicyclic glutarimides
Chang, Meng-Yang,Chen, Chung-Yi,Chen, Shui-Tein,Chang, Nein-Chen
, p. 7547 - 7553 (2003)
We describe an efficient route towards the synthesis of fused bicyclic glutarimides using facile [3+3] reaction of α-sulfonylacetamides with different α,β-unsaturated esters as the key step. Intramolecular cyclization of 4-substituted 3-sulfonylglutarimide to form 5,6-, 6,6- or 6,7-fused bicyclic glutarimides was accomplished via alkylation, oxidative cyclization or ring-closing metathesis in modest yield.
Asymmetric Synthesis of Saturated Hydroxy Fatty Acids and Fatty Acid Esters of Hydroxy Fatty Acids
Mountanea, Olga G.,Limnios, Dimitris,Kokotou, Maroula G.,Bourboula, Asimina,Kokotos, George
, p. 2010 - 2019 (2019)
The recent discovery of a novel class of endogenous lipids, named Fatty Acid esters of Hydroxy Fatty Acids (FAHFAs), that present antidiabetic and anti-inflammatory activities, has attracted the interest on hydroxy fatty acids (HFAs) and their derivatives
Cationic Co(I)-intermediates for hydrofunctionalization reactions: Regio- A nd enantioselective cobalt-catalyzed 1,2-hydroboration of 1,3-dienes
Duvvuri, Krishnaja,Dewese, Kendra R.,Parsutkar, Mahesh M.,Jing, Stanley M.,Mehta, Milauni M.,Gallucci, Judith C.,Rajanbabu
, p. 7365 - 7375 (2019)
Much of the recent work on catalytic hydroboration of alkenes has focused on simple alkenes and styrene derivatives with few examples of reactions of 1,3-dienes, which have been reported to undergo mostly 1,4-additions to give allylic boronates. We find that reduced cobalt catalysts generated from 1,n-bis-diphenylphosphinoalkane complexes [Ph2P-(CH2)n-PPh2]CoX2; n = 1-5) or from (2-oxazolinyl)phenyldiarylphosphine complexes [(G-PHOX)CoX2] (G = 4-substituent on oxazoline ring) effect selective 1,2-, 1,4-, or 4,3-additions of pinacolborane (HBPin) to a variety of 1,3-dienes depending on the ligands chosen. Conditions have been found to optimize the 1,2-additions. The reactive catalysts can be generated from the cobalt(II)-complexes using trimethylaluminum, methyl aluminoxane, or activated zinc in the presence of sodium tetrakis[(3,5-trifluoromethyl)phenyl]borate (NaBARF). The complex, (dppp)CoCl2, gives the best results (ratio of 1,2-to 1,4-addition >95:5) for a variety of linear terminal 1,3-dienes and 2-substituted 1,3-dienes. The [(PHOX)CoX2] (X = Cl, Br) complexes give mostly 1,4-addition with linear unsubstituted 1,3-dienes, but, surprisingly, selective 1,2-additions with 2-substituted or 2,3-disubstituted 1,3-dienes. Isolated and fully characterized (X-ray crystallography) Co(I)-complexes, (dppp)3Co2Cl2 and [(S,S)-BDPP]3Co2Cl2, do not catalyze the reaction unless activated by a Lewis acid or NaBARF, suggesting a key role for a cationic Co(I) species in the catalytic cycle. Regio- A nd enantioselective 1,2-hydroborations of 2-substituted 1,3-dienes are best accomplished using a catalyst prepared via activation of a chiral phosphinooxazoline-cobalt(II) complex with zinc and NaBARF. A number of common functional groups, among them,-OBn,-OTBS,-OTs, N-phthalimido-groups, are tolerated, and er's > 95:5 are obtained for several dienes including 1-alkenylcycloalk-1-enes. This operationally simple reaction expands the realm of asymmetric hydroboration to provide direct access to a number of nearly enantiopure homoallylic boronates, which are not readily accessible by current methods. The resulting boronates have been converted into the corresponding alcohols, potassium trifluororoborate salts, N-BOC amines, and aryl derivatives by C-BPin to C-aryl transformation.
Metal-free one-pot α-carboxylation of primary alcohols
Van Der Heijden, Gydo,Kraakman, Jasper,Biemolt, Jasper,Ruijter, Eelco,Orru, Romano V. A.
, p. 9716 - 9719 (2016)
An efficient metal-free procedure for the formal α-carboxylation of primary alcohols has been developed. The method involves a one-pot oxidation/Passerini/hydrolysis sequence and provides access to α-hydroxy acids bearing a broad range of functional groups. A minor modification to the reaction conditions extends the range of accessible products to α-hydroxy esters.
Chiral geminal disilyl alkane compound, synthesis method and applications thereof
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Paragraph 0204; 0205; 0206; 0207; 0210, (2019/01/14)
The present invention discloses a chiral geminal disilyl alkane compound, which is represented by a formula V, wherein * represents a chiral carbon atom in the formula V. The invention discloses a synthesis method of the chiral geminal disilyl alkane compound, wherein the synthesis method comprises: carrying out a reaction in the presence of a reducing agent by using alkyne represented by a formula I, dihydrosilane represented by a formula II and trihydrosilane represented by a formula III as raw materials and using Xantphos-CoBr2 and a chiral CoX2-OIP complex as catalysts under an inert gas to prepare the chiral geminal disilyl alkane compound represented by the formula V. According to the present invention, the method has characteristics of mild reaction condition, simple operation, highatomic economy, no requirement of the addition of any other toxic transition metals (such as ruthenium, rhodium, palladium and the like) salts, high yield and high enantioselectivity, and has great practical value in the synthesis of drugs and materials, wherein the yield is generally 50-85%, and the enantioselectivity is generally 93-99%. The formulas I, II, III and V are defined in the specification.
Racemic gem disilyl alkane compound containing four silicon-hydrogen bonds, and sybthesis method and application of compound
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Paragraph 0263-0268; 0270, (2019/05/15)
The invention discloses a racemic gem disilyl alkane compound containing four silicon-hydrogen bonds. The compound is as shown in a formula IV. The invention further discloses a synthesis method of the racemic gem disilyl alkane compound. The synthesis method comprises the following step of carrying out a reaction by taking alkyne as shown in a formula I and trihydrosilane as shown in a formula IIas raw materials and taking a chiral CoX-IIP complex as a catalyst in the presence of a reducing agent to obtain the racemic gem disilyl alkane compound containing four silicon-hydrogen bonds, wherein the compound is as shown in the formula IV. The method disclosed by the invention has mild reaction conditions, is simple and convenient to operate and has high atom economy. In addition, the reaction does not need addition of any salts of toxic transition metals (such as ruthenium, rhodium, palladium and the like), and the method has a relatively large practical application value in synthesis of medicines and materials. In addition, the reaction has a medium to excellent yield (51-99%) and high area selectivity (10:1-19:1, most parts larger than 19:1).
Concise synthesis of hydroxy β-methyl fatty acid ethyl esters
Sakai, Yuki,Asakura, Yukiko,Takahashi, Takashi,Morita, Mitsuhiro
, p. 1195 - 1198 (2018/05/02)
Hydroxy β-methyl fatty acid ethyl esters bearing different carbon chain lengths and varying hydroxyl group positions were successfully synthesized from symmetric diols. These fatty acid derivatives are useful intermediates of chemical probes for metabolic
BIPOLAR TETRAETHER LIPIDS
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Paragraph 0423; 0426; 0427, (2017/03/21)
Disclosed herein, inter alia, are compounds, compositions, and liposomes and methods of thereof.
