
Mitsunobu Reaction Using Basic Amines as Pronucleophiles
2017年5月30日 · A novel protocol for extending the scope of the Mitsunobu reaction to include amine nucleophiles to form C–N bonds through the utilization of N-heterocyclic phosphine-butane (NHP-butane) has been developed. Both aliphatic alcohols and benzyl alcohols are suitable substrates for C–N bond construction.
Enantioselective 1,2-Carboamination of 1,3-Dienes with N ...
2024年10月3日 · Sequential regioselective C–C bond and enantioselective C–N bond formation allows rapid assembly of a wide range of value-added chiral allylic amines from readily available N-hydroxyphthalimide (NHP) esters and 1,3-dienes under mild conditions. This developed protocol further demonstrates the versatility and potency of the photoexcited Pd ...
Ligand conjugate SAR and enhanced delivery in NHP
2021年10月6日 · In this study, we synthesized a variety of ligand structures to examine structural aspects of GalNAc ligand design: ligand valency, geometry, linker chemistry, and derivatization of the GalNAc sugar.
amines (e.g. methylaniline (1a)/2,2,4,4-tetramethylpiperidine (2a)) with CO 2 and hydrosilane ([Si]H 2, [Si] ¼ Ph 2Si), catalyzed by 1,3,2-diazaphospholene ([NHP]H). Different from the generally proposed sequential mechanism for the methylation of amine with CO 2, i.e. methylation proceeds via formylation, followed
Formylation or methylation: what determines the chemoselectivity …
2017年9月11日 · The chemoselectivity originates from the competition between the amine and [NHP]H hydride to attack the formyloxy carbon of [Si](OCHO) 2 (the insertion product of CO 2 into [Si]H 2). When the attack of an amine (e.g.1a) wins, the transformation affords formamide (1b) but would otherwise (e.g.2a) result in an N-methylated amine (2c).
甲酰化或甲基化:什么决定了 1,3,2-二氮杂磷烯催化的胺、CO2 和 …
与一般提出的用CO2进行胺甲基化的顺序机制(即甲基化通过甲酰化进行,然后进一步还原甲酰胺得到N-甲基化胺)不同,该研究表征了甲酰化和甲基化之间的竞争机制。 化学选择性源于胺和 [NHP]H氢化物之间竞争攻击 [Si] (OCHO)2(CO2插入 [Si]H2的产物)的甲酰氧基碳。 当胺(例如1a)的攻击获胜时,转化产生甲酰胺(1b),否则(例如2a)会产生N-甲基化胺(2c)。 [Si]H2 或 [NHP]H 对甲酰胺的还原在动力学上是非常不利的,因此我们呼吁关注用于理解胺与 CO2 …
Formylation or methylation: what determines the ... - PubMed
2017年11月1日 · The chemoselectivity originates from the competition between the amine and [NHP]H hydride to attack the formyloxy carbon of [Si](OCHO) 2 (the insertion product of CO 2 into [Si]H 2). When the attack of an amine (e.g.1a) wins, the transformation affords formamide (1b) but would otherwise (e.g.2a) result in an N-methylated amine (2c).
The Asymmetric Synthesis of Amines via Nickel-Catalyzed ...
2021年2月2日 · The NHP esters can be generated in situ from commercially available α-amino acid derivatives and coupled directly, resulting in a straightforward one-pot catalytic enantioselective synthesis of a variety of interesting target molecules.
Formylation or methylation: what determine the chemoselectivity …
The chemoselectivity originates from the competition between amine and [NHP]H hydride to attack formyloxy carbon of [Si](OCHO)2 (the insertion product of CO2 into [Si]H2). When the attack of an amine (e.g. 1a) wins, the transformation affords formamide (1b) and would otherwise (e.g. 2a) result in N-methylated amine (2c).
Decarboxylative Cross-Electrophile Coupling of N-Hydroxyphthalimide …
2016年3月30日 · A new method for the decarboxylative coupling of alkyl N-hydroxyphthalimide esters (NHP esters) with aryl iodides is presented. In contrast to previous studies that form alkyl radicals from carboxy...
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