55500-12-4Relevant academic research and scientific papers
Fast continuous alcohol amination employing a hydrogen borrowing protocol
Labes, Ricardo,Mateos, Carlos,Battilocchio, Claudio,Chen, Yiding,Dingwall, Paul,Cumming, Graham R.,Rincón, Juan A.,Nieves-Remacha, Maria José,Ley, Steven V.
supporting information, p. 59 - 63 (2019/01/11)
A continuous flow method for the direct conversion of alcohols to amines via a hydrogen borrowing approach is reported. The method utilises a low loading (0.5%) of a commercial catalyst system ([Ru(p-cymene)Cl2]2 and DPEPhos), reagent grade solvent and is selective for primary alcohols. Successful methylation of amines using methanol and the direct dimethylamination of alcohols using commercial dimethylamine solution are reported. The synthesis of two pharmaceutical agents Piribedil (5) and Buspirone (25) were accomplished in good yields employing these new methods.
PLANT GROWTH-PROMOTION AGENT AND METHOD FOR PROMOTING PLANT GROWTH
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Paragraph 0139; 0141; 0142; 0143, (2017/11/11)
The present invention concerns: a plant growth-promoting agent comprising a compound represented by Formula (I) or a salt thereof: wherein Ar1 represents a substituted or unsubstituted phenyl group, NZ represents a nitrogen-containing heterocyclic ring group or an acyclic nitrogen-containing group having a partial structure of the nitrogen-containing heterocyclic ring group, n is 0, 1, or 2, R1 and R2 each represent a hydrogen atom, a substituted or unsubstituted C1-3-alkyl group, a cyano group, or a carboxyl group, R1 and R2 may together form an oxo group, and when n is 2, R1 or R2 may be the same or different; and a method for promoting plant growth using the plant growth-promoting agent.
Benzylamines via Iron-Catalyzed Direct Amination of Benzyl Alcohols
Yan, Tao,Feringa, Ben L.,Barta, Katalin
, p. 381 - 388 (2016/01/12)
Benzylamines play a prominent role in numerous pharmaceutically active compounds. Thus, the development of novel, sustainable catalytic methodologies to provide access to these privileged structural motifs is of central importance. Herein we describe a systematic study for the construction of a large variety of benzylamines using a well-defined homogeneous iron complex. The methodology consists of the direct coupling of readily available benzyl alcohols with simpler amines through the borrowing hydrogen methodology, producing a variety of substituted secondary and tertiary benzylamines in moderate to excellent yields for the first time with an iron catalyst. Notably, we explore the versatility of this methodology in the one-pot synthesis of nonsymmetric tertiary amines, sequential functionalization of diols with distinctly different amines, and the synthesis of N-benzyl piperidines via various synthetic pathways. In addition, direct conversion of the renewable building block 2,5-furan-dimethanol to pharmaceutically relevant compounds is achieved.
Reusable supported ruthenium catalysts for the alkylation of amines by using primary alcohols
Peishan, Siah,Dang, Tuan Thanh,Seayad, Abdul Majeed,Ramalingam, Balamurugan
, p. 808 - 814 (2014/03/21)
Efficient and recyclable ruthenium catalysts were synthesized from readily available polystyrene-or silica-supported phosphine ligands. Catalysts bound to the polymer support through an ether linkage showed good to excellent activity towards the N-alkylation of primary and secondary amines to afford the alkylated products in 62-99 % yield at 120-140°C. The supported phosphine ligand/ruthenium ratio was found to be crucial for higher catalytic activity and lower ruthenium leaching. The continuous flow N-alkylation of amines was demonstrated by using the supported catalyst in a column reactor. By adopting the hydrogen-borrowing strategy, the synthesis of the anti-Parkinson agent Piribedil was established in 98 % yield at 140°C. Support group steals the show: An efficient Ru-based heterogeneous catalyst from readily available supported phosphine ligands is developed. The nature of the linkage and the extent of ruthenium incorporation are crucial in determining the catalytic activity. The catalyst can be recycled and used under continuous flow in a packed-bed reactor. The alkylation of cyclic amines is achieved in excellent yield at moderate temperatures in the absence of any external base.
Synthesis of azaspirocycles and their evaluation in drug discovery
Burkhard, Johannes A.,Wagner, Bjoern,Fischer, Holger,Schuler, Franz,Mueller, Klaus,Carreira, Erick M.
supporting information; experimental part, p. 3524 - 3527 (2010/08/06)
(Figure Presented). Make It spirol Readily synthesized heteroatom- substituted spiro[3.3]heptanes generally show higher aqueous solubility than their cyclohexane analogues, and show a trend towards higher metabolic stability. The novel framework can be mo
Non anticholinergic gastric acid secretion inhibitors. New piperazine and related derivatives
Tricerri,Elitropi,Panto,et al.
, p. 555 - 562 (2007/10/08)
Some of the new piperazine derived compounds exhibited interesting gastric antisecretory properties without anticholinergic action. 1 Piperonyl 4 (3,7,11 trimethyl 2,6,10 dodecatrienyl) piperazine was the most active as an antisecretory agent in rat. Some analogous compounds, with the piperazine ring replaced by other heterocyclic or acyclic amines, were also prepared. Structure activity relationships are discussed.
