85356-68-9Relevant academic research and scientific papers
Convergent Synthesis of Immune Inhibitor IMMH002
Chen, Si,Shi, Zeyu,Xiao, Qiong,Yin, Dali
, p. 1174 - 1180 (2020/10/30)
A convergent synthesis of IMMH002 in 36% overall yield starting from bromobenzene is described with a key Suzuki-Miyaura cross-coupling reaction used to provide a crucial intermediate. The route does not require column chromatography and solves the most intractable quality problem caused by a homologue by-product in the original linear synthesis. Furthermore, reducing the use of Lewis acid mediated reactions improves the environmental impact of the synthesis and reduces overall waste. The new route described herein is more efficient, convenient, reliable, and economically more viable when compared to the previously reported linear route.
Preparation method of pusaimode (Chinese name)
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Paragraph 0058-0061, (2020/05/29)
The invention discloses a preparation method of pusaimode. Bromo-benzene is used as an initial raw material to prepare pusaimode by adopting a convergent synthesis route. The yield of the preparationmethod is high, the cost is low, the amount of generated waste water, waste gas, and waste solids is low, the operation is convenient, and the application value is high.
Preparation method of aituomode
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Paragraph 0058-0061, (2020/05/29)
The invention discloses a preparation method of aituomode. Bromo-benzene is used as an initial raw material to prepare aituomode by adopting a convergent synthesis route. The yield of the preparationmethod is high, the cost is low, the amount of generated waste water, waste gas, and waste solids is low, the operation is convenient, and the application value is high.
Preparation method of aituomode
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Paragraph 0050-0053, (2020/05/29)
The invention discloses a preparation method of aituomode. Bromo-benzene and benzene are used as initial raw materials to prepare aituomode by adopting a convergent synthesis route. The yield of the preparation method is high, the cost is low, the amount of generated waste water, waste gas, and waste solids is low, the operation is convenient, and the application value is high.
Migratory Hydrogenation of Terminal Alkynes by Base/Cobalt Relay Catalysis
Liu, Bingxue,Liu, Qiang,Liu, Xufang
supporting information, p. 6750 - 6755 (2020/03/13)
Migratory functionalization of alkenes has emerged as a powerful strategy to achieve functionalization at a distal position to the original reactive site on a hydrocarbon chain. However, an analogous protocol for alkyne substrates is yet to be developed. Herein, a base and cobalt relay catalytic process for the selective synthesis of (Z)-2-alkenes and conjugated E alkenes by migratory hydrogenation of terminal alkynes is disclosed. Mechanistic studies support a relay catalytic process involving a sequential base-catalyzed isomerization of terminal alkynes and cobalt-catalyzed hydrogenation of either 2-alkynes or conjugated diene intermediates. Notably, this practical non-noble metal catalytic system enables efficient control of the chemo-, regio-, and stereoselectivity of this transformation.
Preparation method of pusaimode (Chinese name)
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Paragraph 0049; 0050; 0052, (2020/05/29)
The invention discloses a preparation method of pusaimode. Bromo-benzene and benzene are used as initial raw materials to prepare pusaimode by adopting a convergent synthesis route. The yield of the preparation method is high, the cost is low, the amount of generated waste water, waste gas, and waste solids is low, the operation is convenient, and the application value is high.
Transition-Metal-Free Borylation of Alkyl Iodides via a Radical Mechanism
Liu, Qianyi,Hong, Junting,Sun, Beiqi,Bai, Guangcan,Li, Feng,Liu, Guoquan,Yang, Yang,Mo, Fanyang
supporting information, (2019/07/08)
We describe an operationally simple transition-metal-free borylation of alkyl iodides. This method uses commercially available diboron reagents as the boron source and exhibits excellent functional group compatibility. Furthermore, a diverse range of prim
Selective C(sp3)?H and C(sp2)?H Fluorination of Alcohols Using Practical Auxiliaries
Mao, Yang-Jie,Lou, Shao-Jie,Hao, Hong-Yan,Xu, Dan-Qian
supporting information, p. 14085 - 14089 (2018/10/15)
Selective introduction of fluorine into molecules by the cleavage of inert C?H bonds is of central academic and synthetic interest, yet remains challenging. Given the central role of alcohols in organic chemistry as the most ubiquitous building blocks, a
Ni-Catalyzed Enantioselective Conjunctive Coupling with C(sp3) Electrophiles: A Radical-Ionic Mechanistic Dichotomy
Lovinger, Gabriel J.,Morken, James P.
supporting information, p. 17293 - 17296 (2017/12/15)
The catalytic enantioselective conjunctive coupling of C(sp3) electrophiles can be accomplished with Ni catalysis. The enantioselectivity of the reaction is dependent on reaction mechanism with many substrates able to engage in an asymmetric process with Pybox-Ni complexes, whereas other substrates provide racemic product mixtures. The link between substrate structure and selectivity is addressed.
One-pot preparation of alkyl iodides from esters by indium-catalyzed reductive cleavage of a carbon-oxygen bond
Sakai, Norio,Matsushita, Yohei,Konakahara, Takeo,Ogiwara, Yohei,Hirano, Keisuke
supporting information, p. 1591 - 1595 (2015/03/04)
We describe the indium-catalyzed reductive iodination of aliphatic and aromatic esters with iodine and 1,1,3,3- tetramethyldisiloxane (TMDS). This reducing procedure accommodates a variety of esters, including esters containing alkyl groups, halogens, a hydroxy group, a thioether, and an alkene moiety. Also, this procedure was applied to the cleavage of carbon-oxygen bonds in acrylate polymers.
