On Aug 30, 2017 a scientific literature search for the keywords Biotage AND peptide was performed by Biotage personnel. The search identified 5380 peer-reviewed publications from the global community, excluding patents and simple citations. Below are approximately 100 titles illustrating the breadth and depth of research in which Biotage tools are utilized.
Translated versions of the Safety chapter available in the Biotage® Initiator+ Installation and Safety document (P/N 355976). Languages: Danish, Dutch, Finnish, French, German, Italian, Japanese, Spanish, and Swedish.
The formation of diarylethers by reacting an arylhalide and phenol is usually a reaction demanding long reaction times, high temperatures and strong bases, in order to obtain acceptable yield. The substitution patent of the electrophile and the nucleophile affects the reaction times mostly. A sterically hindered electrophile and a strongly deactivated nucleophile as outlined in the (Scheme 1) below, gives a very low yield (13 %) at conventional reflux for 2 weeks.1,2 Remainder was recovered starting material. We have previously reported the dramatically shortened reaction time to 1 hour along with improved yield running the reaction outlined in the Scheme by heating by microwaves.
User Case: Kissei Pharmaceutical Co., Ltd. One of Japan’s innovative pharmaceutical companies uses Isolera™ flash purification systems and Biotage® Initiator+ microwave synthesizers in the development of new prescription drugs. Modern lab instruments contribute to efficient use of time and resources at Kissei Pharmaceuticals.
User report: Initiator. Prof. Nakamura at the Gakushuin University has described the Initiator as an essential tool for his group’s cutting-edge research. We asked Prof. Nakamura for his views on the latest trends in the fields of organic synthesis and drug discovery.
The rapid synthesis of the non-steroidal anti-inflammatory agent Fenclofenac (2-(2,4-dichlorophenoxy)phenyl acetic acid) under microwave irradiation is reported. Modified reaction conditions of traditional Ullmann ether coupling resulted in high yields of the diaryl ether. The Willgerodt–Kindler transformation and subsequent hydrolysis of thioamide resulted in 52% overall yield of Fenclofenac.
Quinolines are an important class of broad-spectrum antibiotics1 that were traditionally obtained by refluxing an aniline and diethyl ethoxymethylemalonate (Scheme 1) for several hours often in low yield.2 Heating the reaction mixture by microwaves to temperatures above the boiling points, with or without solvents, improves the yields and shortens the reaction time dramatically.3-6
Heck reactions utilizing a thermostable catalyst in combination with microwave irradiation have been performed. A substantial enhancement of reaction rates as well as excellent regiocontrol could be obtained under microwave conditions without using inert gas. A slight increase in yield was also noted.
PNA oligomers have interesting properties such as their increased thermal and chemical stability and resistance to enzymatic degradation which drives their use in various molecular biology, molecular diagnostic, microarray, biosensor and antisense applications. In this study we synthesize two PNA oligomers on a small scale using the Biotage® Initiator+ Alstra™ microwave peptide synthesizer.
The formation of diarylamines by reacting anilines with aromatic electrophiles is, usually, a reaction demanding long reaction times, high temperatures and strong bases, in order to obtain acceptable yield, due to the low nucleophilicity of anilines.1 The Buchwald-Hartwig cross-coupling reaction is a very useable and elegant solution to this problem.2,3,4 Anticipating the classical metal-free SNAr-amination reaction, without using Pd-catalysts and strong bases, with only higher temperature and pressure as tool as depicted in the Scheme below,1 gives no product at all at 180 ºC and very low conversion (9 %) at 220 ºC for 15 minutes when heating by microwaves.5 Remainder was unreacted starting material.
A one-pot process for the preparation of Acyclovir from guanine is described. The key step involves a trimethylsilyl triflate (TfOTMS)-catalysed reaction of silylated guanine with 1,3-dioxalane under microwave irradiation. With this method, the yield is in the same range as with conventional heating, but the speed of the reaction is increased by a factor of 85.