The Experts below are selected from a list of 360 Experts worldwide ranked by ideXlab platform
Jinjia Wang - One of the best experts on this subject based on the ideXlab platform.
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development of a modified process for the kilogram scale synthesis of c met alk inhibitor hs 10168
Organic Process Research & Development, 2017Co-Authors: Jinjia WangAbstract:A modified synthetic route to c-Met/ALK inhibitor HS-10168 has been developed on a kilogram scale. The key steps of the new process include a Suzuki coupling reaction of nitro-containing Bromopyridine 6 and para-phenol boronate 9 to give intermediate 10, which was then converted to its triflate 11. The phosphorus group was introduced by coupling of 11 and dimethylphoshine oxide 8 to give compound 12, which was reduced to produce HS-10168.
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Development of a Modified Process for the Kilogram-Scale Synthesis of c‑Met/ALK Inhibitor HS-10168
2017Co-Authors: Jinjia WangAbstract:A modified synthetic route to c-Met/ALK inhibitor HS-10168 has been developed on a kilogram scale. The key steps of the new process include a Suzuki coupling reaction of nitro-containing Bromopyridine 6 and para-phenol boronate 9 to give intermediate 10, which was then converted to its triflate 11. The phosphorus group was introduced by coupling of 11 and dimethylphoshine oxide 8 to give compound 12, which was reduced to produce HS-10168
Jinkun Huang - One of the best experts on this subject based on the ideXlab platform.
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synthesis of pyrido fused quinazolinone derivatives via copper catalyzed domino reaction
ChemInform, 2016Co-Authors: Meilin Liu, Miaomiao Shu, Chaochao Yao, Guodong Yin, Dunjia Wang, Jinkun HuangAbstract:The copper-catalyzed reaction of isatins (I) with 2-Bromopyridines (II) leads to a variety of pyrido-fused quinazolinones (III).
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synthesis of pyrido fused quinazolinone derivatives via copper catalyzed domino reaction
Organic Letters, 2016Co-Authors: Meilin Liu, Miaomiao Shu, Chaochao Yao, Guodong Yin, Dunjia Wang, Jinkun HuangAbstract:A simple and efficient synthesis of 11H-pyrido[2,1-b]quinazolin-11-ones by Cu(OAc)2·H2O-catalyzed reaction of easily available substituted isatins and 2-Bromopyridine derivatives has been developed. The reaction involves C–N/C–C bond cleavage and two C–N bond formations in a one-pot operation. This methodology is complementary to previously reported synthetic procedures, and two plausible reaction mechanisms are discussed.
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Synthesis of Pyrido-Fused Quinazolinone Derivatives via Copper-Catalyzed Domino Reaction
2016Co-Authors: Meilin Liu, Miaomiao Shu, Chaochao Yao, Guodong Yin, Dunjia Wang, Jinkun HuangAbstract:A simple and efficient synthesis of 11H-pyrido[2,1-b]quinazolin-11-ones by Cu(OAc)2·H2O-catalyzed reaction of easily available substituted isatins and 2-Bromopyridine derivatives has been developed. The reaction involves C–N/C–C bond cleavage and two C–N bond formations in a one-pot operation. This methodology is complementary to previously reported synthetic procedures, and two plausible reaction mechanisms are discussed
Philip Deshong - One of the best experts on this subject based on the ideXlab platform.
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synthesis of the cd ring of the anticancer agent streptonigrin studies of aryl aryl coupling methodologies
Tetrahedron, 2006Co-Authors: William T Mcelroy, Philip DeshongAbstract:A series of functionalized 4-Bromopyridines, representing the C-ring of the anticancer agent streptonigrin have been prepared and their abilities to undergo Pd-catalyzed cross-coupling with streptonigrin D-ring siloxanes were evaluated. The coupling reaction was generally tolerant to the preparation of hindered CD biaryls; however, the electronic effects of both partners play a pivotal role in the success of the coupling process. Analogs of the CD biaryl were prepared by coupling of aryl siloxane derivatives (D-ring component) with highly functionalized 4-Bromopyridines (C-ring); however, the CD biaryl of the natural product could not be prepared in high yield by siloxane coupling due to the facile formation of reduced pyridine under the coupling conditions. Alternatively, the fully functionalized CD biaryl of streptonigrin was prepared using a Suzuki coupling of appropriately functionalized C-ring bromide and D-ring aryl boronic acid. The described approach is highly convergent and readily amenable to the synthesis of analogs.
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siloxane based cross coupling of Bromopyridine derivatives studies for the synthesis of streptonigrin and lavendamycin
Organic Letters, 2003Co-Authors: William T Mcelroy, Philip DeshongAbstract:Highly functionalized 4-Bromopyridines were prepared and found to undergo fluoride-promoted, Pd-catalyzed cross-coupling with aryltrialkoxysilanes to give sterically demanding biaryls. The 3-nitro-4-Bromopyridine derivative coupled in good yield with TBAT (tetrabutylammonium triphenyldifluorosilicate) to provide a biaryl adduct that serves as a model system for the total synthesis of the antitumor antibiotics streptonigrin and lavendamycin.
Guijie Li - One of the best experts on this subject based on the ideXlab platform.
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cucl catalyzed ullmann type c n cross coupling reaction of carbazoles and 2 Bromopyridine derivatives
Journal of Organic Chemistry, 2017Co-Authors: Xiangdong Zhao, Kun Fang, Guijie LiAbstract:A CuCl-catalyzed Ullmann-type C–N cross-coupling reaction of carbazoles and 2-Bromopyridine derivatives has been developed for the synthesis of N-heteroarylcarbazole derivatives employing 1-methyl-imidazole and t-BuOLi as ligand and base, respectively, both of which are found to significantly promote the reaction. Low cost and low loading of both catalyst and ligand, together with high reaction yields, render this practical reaction to be suitable for large-scale preparations and could be useful in material science.
Meilin Liu - One of the best experts on this subject based on the ideXlab platform.
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synthesis of pyrido fused quinazolinone derivatives via copper catalyzed domino reaction
ChemInform, 2016Co-Authors: Meilin Liu, Miaomiao Shu, Chaochao Yao, Guodong Yin, Dunjia Wang, Jinkun HuangAbstract:The copper-catalyzed reaction of isatins (I) with 2-Bromopyridines (II) leads to a variety of pyrido-fused quinazolinones (III).
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synthesis of pyrido fused quinazolinone derivatives via copper catalyzed domino reaction
Organic Letters, 2016Co-Authors: Meilin Liu, Miaomiao Shu, Chaochao Yao, Guodong Yin, Dunjia Wang, Jinkun HuangAbstract:A simple and efficient synthesis of 11H-pyrido[2,1-b]quinazolin-11-ones by Cu(OAc)2·H2O-catalyzed reaction of easily available substituted isatins and 2-Bromopyridine derivatives has been developed. The reaction involves C–N/C–C bond cleavage and two C–N bond formations in a one-pot operation. This methodology is complementary to previously reported synthetic procedures, and two plausible reaction mechanisms are discussed.
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Synthesis of Pyrido-Fused Quinazolinone Derivatives via Copper-Catalyzed Domino Reaction
2016Co-Authors: Meilin Liu, Miaomiao Shu, Chaochao Yao, Guodong Yin, Dunjia Wang, Jinkun HuangAbstract:A simple and efficient synthesis of 11H-pyrido[2,1-b]quinazolin-11-ones by Cu(OAc)2·H2O-catalyzed reaction of easily available substituted isatins and 2-Bromopyridine derivatives has been developed. The reaction involves C–N/C–C bond cleavage and two C–N bond formations in a one-pot operation. This methodology is complementary to previously reported synthetic procedures, and two plausible reaction mechanisms are discussed
