Pseudo-ephedrine

With Phenylpropanolamine at hand (or ephedrine and pseudo-ephedrine) one would next need to reduce that alpha carbon OH group to get the final amine. Strike understands that the current favorite methods for doing this involve lithium and amine. HI and red P or other iodine related protocols. So when you meth heads ruin every aspect of those methods as well, what will you do then The following are a couple of OH reduction methods (Strike thinks) that have applicable use [99-100]. 

Likewise, record the second derivative spectra of the four standard pseudo-ephedrine hydrochloride solutions and record the peak heights DL at 258-259 nm plot the results against concentration and confirm that a straight line is obtained. 

Alka-Seltzer Plus Cold and Flu Liqui-Gels—dextromethorphan HBr, pseudo ephedrine HC1, acetaminophen... 

From calculations of the preferred conformation of the ephedrine and pseudo ephedrine molecules the topography of the adrenergic receptor as a flat surface has been deduced (26). This view, however, does not explain the decisive effect of the additional methyl group its relative position should not influence the interaction with the proposed receptor to a large extent (Fig. 7a). However, as the differences in activities are especially high for the ephedrine and pseudo ephedrine isomers, we believe that the receptor must have an intercalated structure similar as projected for the "binding sites" of the silicones (Fig. 7b). ... 

Operational activities have continued under Project Prism, the international initiative designed to address diversion of the five main precursors used in the illicit manufacture of amphetamine-type stimulants, namely, ephedrine, 3,4-methylene-dioxyphenyl-2-propanone (3,4-MDP-2-P), l-phenyl-2-propanone (P-2-P), pseudo-ephedrine and safrole, as well as the equipment used in such illicit manufacture. Activities during 2004 have focused on launching operations to address weaknesses in control and monitoring mechanisms identified during 2003, such as monitoring... 

Clearly, upon using the enantiomeric catalyst [(S,S) instead of (R,R)] the opposite enantioselectivity of the overall process results. However, this effect is also seen with catalysts that are of analogous configuration, but not derived from trans-1,2-diaminocyclohexane (DACH). For example, the pseudo-ephedrine derived catalyst shown in Scheme 5, having (5)-configuration at the centers of chirality, shows some preference for the (5)-azlactone kinetically favors the (5)-azlactone in alcoholytic ring opening [37]. 

Scheme 5 Pseudo-ephedrine derived catalyst which favors the ring opening of ( S)-azlactones...

Nasal formulations of modern sympathicomimet-ics like oxymetazoline and xylometazoline are effective. Rebound nasal congestion after withdrawal of sympathicomimetic-containing nose sprays or drops is a common phenomenon and patients should be advised to use these medicaments no longer than 3-5 days. Older per oral drugs like ephedrine and pseudo-ephedrine have no place in the therapy of rhinitis due to the risk of serious adverse reactions which are not in proportion to the indication. 

Methamphetamine, a Schedule 11 drug, was first synthesized in 1919. It can be synthesized from ephedrine or pseudo-ephedrine. Methamphetamine is available by prescription for weight control, ADHD, and narcolepsy under the brand name Desoxyn . Street names for methamphetamine include chalk, crank, crystal, fire, glass, ice, rocks, shabu, speed, and yaba. Methamphetamine is often found at rave sites, where people exert themselves while dancing and deprive themselves of sleep, food, and drink, which can result in increased body temperature with excessive sweating and possibly a salt imbalance. 

Global seizures of ATS continue to be dominated by seizures of methamphetamine. Over the 2000-2005 period, 49 per cent of ATS seizures were in the form of methamphetamine, 15 per cent in the form of amphetamine, and 14 per cent in the form of ecstasy. The trend in recent years, however, has been towards rising proportions of amphetamine and falling proportions of methamphetamine, reflecting improved control over the two main methamphetamine precursors, ephedrine and pseudo-ephedrine. 

Ephedrine and pseudo-ephedrine, sufficient to produce some 28 mt of methamphetamine ... 

Board (INCB), was informed of some 1,900 shipments involving ephedrine and pseudo-ephedrine between November 2004 and October 20055. Between November 2005 and October 2006, over 2,200 shipments of ATS precursors were monitored. This resulted in 99 detailed investigations, including 40 cases involving 165 mt of ephedrine and pseudo-ephedrine that were interdicted or suspended. 6... 

This is reflected in the declining number of seized methamphetamine labs, from 17,199 in 2004 to 12,144 in 2005. Precursor control has also had a positive impact. Pseudo-ephedrine seizures in North America fell dramatically from a record 174.4 mt in 2004 to 0.6 mt in 2005. Ephedrine seizures also declined from 2.1 to 1.4 mt 9. Expressed in ATS equivalents, the precursors seized in 2004 would have been sufficient to produce 118 mt of methamphetamine those seized in 2005 would have been sufficient to produce only 1.3 mt.10... 

The USA also reduced the availability of over-the-counter (OTC) pharmaceutical preparations containing ATS precursors, notably pseudo-ephedrine. Similar controls in Canada (since 2003) reduced the flow of OTC preparations containing pseudo-ephedrine across the border. These efforts squeezed out large numbers of kitchen labs, and thus led to less US laboratory seizures in 2005 - a trend which appears to have continued in... 

Role of Project PRISM in countering synthetic drugs and their precursors , INCB presentation to the Conference Europe-Asia Cooperation on Synthetic Drugs and their Precursors , Paris, 6-7 March 2007. These are substantial amounts. By comparison, total licit trade in ephedrine and pseudo-ephedrine is estimated at around 30 mt and 1,200 mt respectively. [Source INCB, 2005 Precursors]. The 16 mt of interdicted/suspended shipments could have been used to produce 110 mt of methamphetamine. Were this to have ended up on the illicit market, it would have increased global methamphetamine production by some 40 per cent. 

Amphetamine/methamphetamine precursor (P2P seized in USA) ] Amphetamine precursors (P2P, phenylacetic acid, norephedrine) I Methamphetamine precursors (pseudo-ephedrine, ephedrine) Trend... 

Taking North America as a whole, the declines in the USA were partly offset by rising production in a few super-labs in Mexico. The number of methamphetamine laboratories dismantled in Mexico rose from 10 in 2002 to 18 in 2004 and 34 in 2005. Until recently pseudo-ephedrine and ephedrine were fairly readily available in the country. The Mexican authorities, however, have recently taken measures to counter the diversion of the two chemicals. These efforts reduced the import of ephedrine and pseudo-ephedrine by 40 per cent in 2005 (to 133 mt), with a further reduction of almost 50 per cent (to about 70 mt) expected for 2006.13... 

B National Drug Intelligence Centre, National Drug Threat Assessment 2007, Oct. 2006 According to data collected by the INCB, the decline was from 177-8 mt of pseudo-ephedrine in 2004 to 107.7 mt in 2005 and from 118 kg ephedrine in 2004 to 64 kg in 2005, which is also equivalent to an overall decline of about 40 per cent. 

A further, indirect indication of methamphetamine production can be derived from the geographical location of ephedrine and pseudo-ephedrine seizures. The largest such seizures in Asia over the 2004-2005 period were reported from China (which is also one of the main licit producers of ephedrine and pseudo-ephedrine), followed by the Philippines, Myanmar, Indonesia and India (another major licit producer of ephedrine and pseudo-ephedrine), and at far lower levels, Hong Kong SAR of China and Thailand. Taken together, the Asian countries accounted for 89 per cent of the world s ephedrine and pseudo-ephedrine seizures in 2005.20... 

Europe as a whole accounted for about 6 per cent of global ephedrine seizures over the 2004-2005 period. Listed in order of importance, the following European countries reported seizures of methamphetamine precursors over the same period the Czech Republic, Greece, the Russian Federation, the UK, Bulgaria, Germany, Iceland, Romania, Hungary, Slovakia, the Ukraine, France, Norway and Latvia. In 2006, EUROPOL noted increased export, transshipment and diversion of ephedrine and pseudo-ephedrine to the European Union.24... 

Methamphetamine production is becoming a problem in South Africa. This is also reflected in demand indicators, notably in Cape Town. The number of dismantled methamphetamine labs has been rising steadily, from only 1 in 2002 to 4 in 2004 and 11 in 2005. Both ephedrine and pseudo-ephedrine, mainly originating in China, are now being seized in the country. Thus far there are no indications that methamphetamine is produced for export. 

Y. M. Liu and S. J. Sheu, Determination of ephedrine and pseudo-ephedrine in Chinese herbal preparations by capillary electrophoresis, J. Chromotogr., 637 219 (1993). 

Various molecules were considered for studying the influence of the five-mem-bered ring conformations, and of the bulkiness of the ring substituents on the dia-stereomeric excess of the aminated products. Optically active (+)-ephedrine 89a and (—)-pseudo-ephedrine 89b were chosen as the chiral amino alcohols because of their relatively low cost and in view of the excellent results obtained in the similar asymmetric synthesis of a-amino carboxylic acids [13]. 

Ma Huang has an anti-inflammatory activity (598). A survey for the active principle in the crude drug demonstrated that the most active one is pseudo-ephedrine. Ephedroxane was also isolated as a minor anti-inflammatory principle. The mechanism of the anti-inflammatory action of these compounds does not involve the central nervous system. Of several mechanisms considered, inhibition of prostaglandin E2 biosynthesis may be of great importance (398). 

Chiral Auxiliary Used for Asymmetric Ti-ansformations (Thermodynamic Control). Racemic iV-benzyl-iV-methyl-a-amino propiophenone mixed with (2R,3R)-DPTA in acetone or dichloromethane leads with 90% yield to the corresponding salt of the (S)-amino ketone, which was reduced over Palladium on Carbon to a mixture of ephedrine (80%) and pseudo-ephedrine (20%) (eq 8). ... 

In addition to the R and S designations, compounds with two chiral centers may also be identified by stereochemical nomenclature that describes the entire system. For example, the erythro and threo nomenclature derived from carbohydrate chemistry may be employed to describe the relative positions of similar groups on each chiral carbon. Thus, the ephedrines are designated as erythro forms since the similar groups (OH and NHCH3) are on the same side of the vertical axis of the Fischer projection, and the pseudo-ephedrines are designated as threo forms since like groups are on opposite sites of the vertical axis of the projection (Fig. 10). 

FIGURE 26.4 Preferred conformations of D-(—)-ephedrine and of D-(—)-pseudo-ephedrine. 

Quantum mechanical calculations on the conformational properties of norepinephrine have also been reported. Interconversion of ephedrine and pseudo-ephedrine to a slight extent under y-irradiation has been observed. Absorption of carbon dioxide by cupric ephedrinates can be accounted for by carbamate formation rather than formation of metal-carbon dioxide bonds. -Acylation of /3-phenethylamines by protected amino-acids, e.g. N-CBZ-leucine, has been reported. ... 

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